AbMole Inhibitor catalog July 2014

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PI3K/Akt/mTOR
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PI3K/Akt/mTORFree Sample Program
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us by info@abmole.com!

1
Table of Contents
PI3K/Akt/mTOR PI3K....................................................................1
mTOR.................................................................4
Akt ......................................................................3
GSK-3.................................................................6
PDK1 ..................................................................6
S6 Kinase ...........................................................7
AMPK .................................................................7
DNA-PK..............................................................7
Protein Tyrosine Kinase VEGFR/PDGFR..................................................7
EGFR/HER2.......................................................10
c-Met ..................................................................12
IGF-1R................................................................14
ALK.....................................................................13
Angiogenesis FLT3 ...................................................................15
Src-bcr-Abl .........................................................15
Syk .....................................................................16
HIF......................................................................15
BTK ....................................................................16
FAK ....................................................................16
Apoptosis Bcl-2 ..................................................................17
p53 ....................................................................17
TNF-alpha ..........................................................17
Caspase ............................................................18
Mdm2 .................................................................18
IAP......................................................................18
JAK/STAT JAK.....................................................................19
Pim .....................................................................20
STAT ..................................................................20
MAPK MEK....................................................................20
p38 MAPK ..........................................................21
Raf......................................................................22
JNK.....................................................................22

PI3K/Akt/mTOR
2
Cytoskeletal Signaling HSP90 ................................................................23
Kinesin................................................................25
Wnt/beta-catenin ................................................25
Microtubule.........................................................24
Integrin ...............................................................25
Cell Cycle Aurora Kinase.....................................................26
CDK....................................................................27
Checkpoint .........................................................28
PLK.....................................................................29
ROCK.................................................................29
Wee1 ..................................................................29
TGF-beta/Smad TGF-beta ............................................................30
PKC....................................................................30
DNA Damage HDAC ................................................................31
PARP..................................................................33
ATM/ATR............................................................34
DNA/RNA Synthesis...........................................34
Topoisomerase...................................................35
Sirtuin .................................................................36
Epigenetics Epigenetic Reader Domain ................................ 36
Histone demethylases ........................................36
DNA Methyltransferase ......................................36
Histone Methyltransferase .................................
Stem Cells & Wnt Hedgehog...........................................................37
NF-κB NF-κB ................................................................. 37
IκB/IKK ............................................................... 37

Neuronal Signaling 5-HT Receptor....................................................38
COX....................................................................38
GluR ...................................................................39
Gamma-secretase..............................................39
Histamine Receptor............................................40
P2 Receptor .......................................................40
GABA Receptor..................................................39
BACE..................................................................39
GPCR & G Protein Cannabinoid .......................................................40
CXCR .................................................................40
OX Receptor.......................................................41
SGLT ..................................................................41
Endothelin Receptor...........................................41
Endocrinology & Hormones GPR....................................................................42
Estrogen Receptor .............................................42
Androgen Receptor ............................................42
Transmembrane Transporters Sodium Channel.................................................43
P-gp....................................................................43
ATPase...............................................................43
Potassium Channel ............................................43
CFTR...................................................................43
Metabolism PPAR..................................................................45
CYP17 ................................................................44
PDE....................................................................45
CETP..................................................................44
HMG-CoA...........................................................45
Transferase ........................................................45
Dehydrogenase ..................................................44
Factor Xa............................................................44
Monoamine Oxidase ..........................................45

PI3K/Akt/mTOR
2
Proteases Proteasome ........................................................47
Aminopeptidase..................................................46
DPP-4.................................................................46
Deubiquitinase....................................................46
HCV Protease ....................................................47
Microbiology Integrase ............................................................49
CCR....................................................................48
HIV Protease ......................................................48
Reverse Transcriptase .......................................49
Others PKA ....................................................................50
LHRH/GnRH.......................................................50
TRPV..................................................................51
Angiotensin Receptor .........................................49
Autophagy ..........................................................49
CGRP Receptor .................................................50
Liver X Receptor.................................................50
Farnesoid X Receptor ........................................50
Others.................................................................51

PI3K/Akt/mTOR
PPII33KK I nInhihbiibtoirtsors
M1651 AS605240
AS-605240 is a potent and selective
inhibitor of PI 3-kinase γ (PI3Kγ) with
an IC50 of 8 nM.
Size:
10mg 50mg 200mg >1000mg Inquiry
M1671 BEZ235 (NVP-BEZ235)
HOT
BEZ235 (NVP-BEZ235) is a potent dual
PI3K and mTOR inhibitor of p110α, p110γ,
p110δ and p110β with IC50 of 4 nM, 5 nM,
7 nM and 75 nM, respectively.
Size:
HOT
M1680 BKM120 (NVP-BKM120)
BKM120 (NVP-BKM120) is a potent and
highly specific oral pan-class I PI3K inhibitor.
Size:
HOT
M1715 GDC-0941
GDC-0941 is a potent inhibitor of PI3Kα/δ
with IC50 of 3 nM, with modest selectivity
against p110β (11-fold) and p110γ (25-fold).
Size:
M2220 GDC-0941 Bimesylate
GDC-0941 Bimesylate is the orally
bioavailable bismesylate salt of a
potent inhibitor PI3K.
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M1727 GDC-0980 (RG7422)
GDC-0980(RG7422) is a potent,
highly selective, oral, dual inhibitor
of class I PI3K and mTOR.
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M1735 BGT226 (NVP-BGT226)
BGT226(NVP-BGT226) is a novel
phosphoinositide 3-kinase/mTOR
dual inhibitor.
Size:
10mg 50mg >200mg Inquiry
M1736 CH5132799
CH5132799 is a novel and potent
class I PI3K inhibitor with IC50
value of 0.014 μM.
Size:
M1739 PKI-179
PKI-179 is an orally dual phosph
-atidylinositol-3-kinase (PI3K)/
mammalian target of rapamycin
(mTOR) inhibitor with potential
antineoplastic activity.
Size:
M1770 PIK-75 Hydrochloride
PIK-75 Hydrochloride is a PI3K
p110α specific inhibitor with
IC50s of 6,1300,76,510 nM
for p110α,p110β,p110γ, p110δ
respectively.
Size:
M1772 PKI-587 (PF-05212384)
PKI-587(PF-05212384) is a highly
potent dual PI3K/mTOR kinase
inhibitor with the IC50 value of
0.4nM.
Size:
M1773 PI-103
PI-103 is a potent, ATP-competitive
PI3K,cell-permeable,inhibitor.The
IC50 values are 2, 8, 20, 26, 48, 83,
88,150nM for DNA-PK, p110α, mTORC1,
PI3-KC2β, p110δ, mTORC2, p110β,
and p110γrespectively.
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PI3K/Akt/mTOR
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www.abmole.com ● Shop Online info@abmole.com 1

PI3K/Akt/mTORPI3K/Akt/mTOR
1
M1788 IC87114 (PIK-293)
IC87114 is a compound that inhibits
the p110δ isoform of PI3K selectively,
p110δ (IC50 = 0.13 μM) vs. p110α
(IC50 = 200 μM), p110β(IC50 = 16 μM)
and p110γ(IC50 = 61 μM).
Size:
M1795 TGX-221
TGX-221 is a potent and specific cell
permeable inhibitor of PI3K,p110β
(IC50 = 10nM).
Size:
M1809 NU7441 (KU 57788)
NU7441 (KU 57788) is a potent and
selective DNA-dependent protein
kinase (DNA-PK) inhibitor with IC50
values of 14, 1700, 5000,>100000
and >100000 nM for DNA-PK, mTOR,
PI 3-K, ATM and ATR respectively.
Size:
M1819 A66
A66 is a potent and specific inhibitor
of PI3K p110α with IC50 values of 32,
30 and 43 nM for p110α, p110α/E545K
and p110α/H1047R.
Size:
M1849 XL765 (SAR245409)
XL765 is a PI3K/mTOR dual kinase
inhibitor with IC50 values of 157 nM,
39 nM, 113 nM, 9 nM and 43
nM for mTOR, p110α, p110β,
p110γ and p110δ, respectively.
Size:
M1878 ZSTK474
ZSTK474 is an ATP-competitive inhibitor
of PI3K, induces G1 arrest of the cell cycle
in vivo.
Size:
M1879 XL147 (SAR245408)
XL147 (SAR245408) is an orally
selective small molecule Class I
PI3K kinase family inhibitor.
Size:
M1886 TG100-115
TG100-115 is a selective PI3K γ/δ
inhibitor with IC50 values of 83 and
235 nM respectively.
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M1896 PIK-90
PIK-90 is a novel and potent PI3K
inhibitor with IC50 values of 11 nM,
350 nM, 18 nM and 58 nM for p110α,
p110β, p110γ and p110δ respectively.
Size:
M1925 LY294002
LY294002 is a highly selective PI3K
inhibitor with IC50 values of 0.31, 0.73,
1.06 and 6.60μM for PI3Kβ, PI3Kα, PI3Kδ
and PI3Kγ respectively.
Size:
M1931 GSK2126458
GSK2126458 is a highly potent inhibitor
of PI3K and mTOR with low picomolar
to subnanomolar activity.
Size:
M1933 GNE-493
GNE-493 is a potent, selective and
orally available pan-PI3-kinase and
dual pan-PI3-kinase/mTOR inhibitor
for the treatment of cancer.
Size:
2 info@abmole.com www.abmole.com ● Shop Online
PI3K/Akt/mTOR
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PI3K/Akt/mTOR
PI3K/Akt/mTOR
HOT
MP1P9II343K5K I nICnhAihbLii-bt1oi0rts1o r(GsS-1101)
CAL-101 (GS-1101) is an oral PI3Kδ
-specific inhibitor that has shown
preclinical and clinical activity in non
-Hodgkin lymphoma and chronic
lymphocytic leukemia.
Size:
M1978 GSK1059615
GSK1059615 is a potent, ATP-competitive
inhibitor of PI 3-kinase alpha (PI3Kα) with
IC50 of 2 nM.
Size:
M1984 PF-04691502
PF-04691502 is a potent and selective,
ATP-competitive PI3K/mTOR inhibitor
with IC50 of 7.5 nM and 3.8 nM of AKT
T308 and AKT S473, respectively.
Size:
HOT
M2050 GSK2636771
GSK2636771 is a potent, orally available
and specific PI3K p110β(PI3K beta,PI3Kβ)
inhibitor.
Size:
M2053 Wortmannin (SL-2052)
Wortmannin is a specific, covalent
inhibitor of phosphatidylinositol 3
-kinase(PI 3-kinase) with IC50 of
3 nM.
Size:
M2073 IPI-145
IPI-145 is a potent, oral inhibitor of PI3K
delta and PI3K-gamma.
NEW
M2104 BYL719
BYL719 is the first oral PI3K
inhibitor that strongly and
selectively inhibits the PI3K
alpha isoform of PI3K.
Size:
HOT
M2135 GDC-0032
GDC-0032 is a potent, next
generation PI3-kinase inhibitor.
Size:
NEW
M2295 AZD6482
AZD6482 is an inhibitor of PI3Kβ
with IC50 of 21 nM.
Size:
M2296 3-Methyladenine (3-MA)
3-Methyladenine (3-MA) is a selective PI3K
inhibitor for Vps34 and PI3Kγ with IC50 of
25 μM and 60 μM, respectively.
Size:
APIk3tK I Innhhiibbiitotorsrs
M1654 AT7867
AT7867 is a potent and oral inhibitor of
AKT and p70 S6 kinase with an IC50 of
17 nM.
Size:
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HOT
M1789 GSK690693
GSK690693 is a potent Akt inhibitor
(Akt1 IC50= 2 nM, Akt2 IC50 = 13 nM,
Akt3 IC50 = 9 nM).
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1
M1823 Perifosine (KRX-0401, NKA17)
Perifosine is an orally active Akt inhibitor, the antiproliferative
properties of Perifosine with an IC50 of 0.6–8.9 μM.
Size:
M1837 MK-2206
MK-2206 is a novel allosteric inhibitor of
Akt with IC50 values of 8 nM, 12nM and
65nM for Akt1, Akt2 and Akt3, respectively.
Size:
10mg 50mg 200mg >1000mg Inquiry M1666 AZD8055
M1862 GDC-0068 (RG7440)
GDC-0068 (RG7440) is a potent and selective,
ATP-competitive Akt inhibitor with IC50 values
of 5 to 18 nM.
Size:
M1884 Triciribine (API-2, NSC 154020, TCN)
Triciribine (API-2, NSC 154020) is a selective
inhibitor of Akt (protein kinase B) signaling
with IC50 of 130 nM.
M2132 A-674563
A-674563 is a potent, orally available PKB
/Akt inhibitor with an IC50 of 14 nM.
Size:
AZD8055 is a novel ATP-competitive
inhibitor of mTOR kinase with an IC50
of 0.8 nM.
Size:
M1703 Deforolimus (Ridaforolimus, AP23573)
Deforolimus (also known as AP23573 and MK-8669) is an
investigational targeted and small-molecule mTOR inhibitor.
Size:
M1709 Everolimus (RAD001, Certican)
Everolimus (RAD001) also known as SDZ-RAD and Certican is
an mTOR inhibitor with IC50 of 0.63 nM.
Size:
PI3K/Akt/mTOR
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M1900 PHT-427
PHT-427 is a novel dual Akt and PDPK1 inhibitor
(Ki of 2.7 μM and 5.2 μM respectively).
Size:
M2303 AZD5363
AZD5363 is a potent Akt inhibitor for Akt1,
Akt2 and Akt3 with IC50 of 3 nM, 8 nM
and 8 nM, respectively.
Size:
mPIT3KO IRnh Iinbihtoirbsitors
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PI3K/Akt/mTOR
PI3K/Akt/mTOR
MP1P7II333K1K I nIKnhUihb-i0ibt0oi6rts3o7r9s4 (GS-1101)
KU-0063794 is a potent and selective
mTOR inhibitor with IC50 values of
approximately 10 nM for mTORC1
and mTORC2.
Size:
HOT
M1755 WYE-354
WYE-354 is a cell-permeable pyrazolopyrimidine
compound that acts as a potent and ATP
competitive mTOR inhibitor (IC50 = 5 nM
with S6K as the substrate and 100 μM ATP).
Size:
M1756 WYE-687
WYE-687 is a novel ATP-competitive and
selective inhibitors of the mammalian target
of rapamycin(mTOR) with an IC50 of 7 nM.
Size:
M1760 Palomid 529 (P529)
Palomid 529(P529) is a novel potent PI3K/Akt/mTOR inhibitor
and shows a potent antiproliferative activity in the NCI-60 cell
lines panel, with growth inhibitory 50
(GI50) <35 μM.
Size:
M1768 Rapamycin (Sirolimus, Rapamune)
Rapamycin(Sirolimus,Rapamune)
is an inhibitor of mTOR.The
mammalian target of rapamycin
(mTOR) is a kinase responsible for
mitogen-induced cell proliferation
/survival signaling.
Size:
M1852 WAY-600
WAY-600 is a selective single digit
nanomolar ATP-competitive mTOR
inhibitor with an IC50 of about 9 nM.
HOT
M2022 Torin 2
Torin 2 is a potent and selective
mTOR inhibitor with IC50 of 2.1nM.
Size:
M2094 GDC-0349 (RG7603)
GDC-0349 is a potent and selective,
ATP-competitive mTOR inhibitor.
Size:
M2099 OSI-027
OSI-027 is an orally bioavailable,
potent and selective inhibitor of
mTORC1 and mTORC2 with
IC50 values of 22 nM and 65
nM, respectively.
Size:
M2118 XL388
XL388 is a novel, highly potent, ATP-competitive and orally
bioavailable mTOR inhibitor.
Size:
5mg 10mg 25mg 50mg >100mg Inquiry
NEW
M2151 INK128 (MLN0128)
INK128(MLN0128) is a potent and selective
dual TORC1/2 inhibitor with IC50 of 1 nM.
Size:
Size:
NEW
M1981 PP242
PP242 is a selective, ATP-competitive
mTORC1/mTORC2 inhibitor with IC50
of 8 nM.
Size:
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1
M2299 AZD2014
AZD2014 is a novel dual mTORC1
and mTORC2 inhibitor with potential
Size:
M1692 CHIR-99021 (CT99021)
CHIR-99021 is an aminopyrimidine
derivative that inhibits GSK3α and
GSK3β with IC50 values of 10 and
6.7 nM, respectively.
Size:
NEW
M1848 OSU-03012
OSU-03012 is a novel and potent
inhibitor of PDK-1 with an IC50 of
5 μM.
Size:
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PI3K/Akt/mTOR
M2061 SB 216763
SB216763 is a potent and selective,cell
permeable glycogen synthase kinase-3
(GSK-3) inhibitor with an IC50 value of
34 nM for GSK-3α.
Size:
M2304 TWS119
TWS119 is a GSK-3β inhibitor
with IC50 of 30 nM.
Size:
M2178 AZD2858
AZD2858 is a potent, orally bioactive
inhibitor of GSK-3.
Size:
PPDI3KK 1In hInibhitiobristors
GPIS3KK I-n3h Iibnihtoirbsitors
M1989 CHIR-99021 hydrochloride
CHIR-99021 HCl is a hydrochloride of CHIR-99021, with IC50
of 10 nM and 6.7 nM for GSK-3α and GSK-3β, respectively.
Size:
Size:
M2184 Indirubin
Indirubin is a potent cyclin-dependent kinases
and GSK-3β inhibitor with IC50 of ~75 nM
and 0.19 μM.
M2305 CHIR-98014
CHIR-98014 is a potent and
selective GSK-3 inhibitor for
GSK-3ɑ and GSK-3β with
IC50 of 0.65 nM and 0.58nM,
respectively.
Size:
M2306 Tideglusib (NP031112, NP-12)
Tideglusib (NP031112, NP-12) is a
potent non ATP-competitive inhibitor
of GSK3 with IC50 of 60 nM.
Size:
M2115 GSK2334470
GSK2334470 is a highly specific
and potent inhibitor of PDK1 with
IC50 of 10 nM.
Size:
M2310 BX795
BX795 is a potent and specific TBK1, IKKε and PDK-1 inhibitor
with IC50 of 6 nM, 41 nM and 111 nM, respectively.
NEW
NEW
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Protein Tyrosine Kinase
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MP2P3II313K1K I nIBnhXihb-9iibt1o2irtsors
BX912 is a selective potent PDK1 inhibitor with IC50 of 12 nM.
Size:
SP6I3 KK Iinnhaibsieto rIns hibitors
M1948 BI-D1870
BI-D1870 is a small molecule specific
inhibitor of the p90 RSK (ribosomal
S6 kinase) with an IC50 of 10-30 nM.
Size:
M2271 PF-4708671 (PF-04708671)
PF-4708671 is a novel cell-permeable
inhibitor of S6K1 with Ki/IC50 value of
20 nM/160 nM.
VPEI3GK FInRhi/bPitDorGsFR Inhibitors
M1640 ABT-869 (Linifanib)
ABT-869 (Linifanib) is an ATP
-competitive,multi-targeted RTK
inhibitor that is completely
effective against all members
of VEGFR and PDGFR.
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M1643 AEE788 (NVP-AEE 788)
AEE788 (NVP-AEE788) is a novel multitargeted
HER 1/2 and VEGFR 1/2 receptor family tyrosine
kinases inhibitor with IC50 of 2, 6, 77, 59 nM for
EGFR, ErbB2, KDR, and Flt-1.
Size:
M1656 AV-951 (Tivozanib)
AV-951 (Tivozanib) is a potent VEGFR-1, 2 and 3, c-Kit and PDGFR
inhibitor with IC50 of 0.21, 0.16, 0.24, 1.63 and 1.72 nM respectively.
Size:
NEW
APIM3KP IKnh Iinbihtoibrsitors
M2238 Dorsomorphin dihydrochloride
Dorsomorphin dihydrochloride is a
otent and selective AMPK inhibitor
with Ki value of 109 nM.
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DPIN3KA -InPhKib iItnorhsibitors
NEW
M2308 NU7026
NU7026 is a DNA-PK inhibitor with
IC50 of 0.23 μM.
Size:
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M1658 Axitinib (AG-013736)
Axitinib (AG013736) inhibits
multiple targets including
VEGFR, PDGFR and cKit.
HOT
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M1669 Regorafenib (BAY 73-4506)
Regorafenib (BAY 73-4506) is a novel oral
multikinase inhibitor of c-KIT, VEGFR2,B-Raf
with IC50s of 17, 40 and 69 nM respectively.
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M1673 BIBF1120 (Vargatef)
BIBF 1120 (Vargatef) is a novel triple
angiokinase inhibitor of VEGFR, PDGFR
and FGFR.
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PI3K/Akt/mTORProtein Tyrosine Kinase
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M1838 Masitinib (AB1010)
Masitinib is a tyrosine kinase inhibitor targeting stem cell factor
receptor (c-kit) and platelet-derived growth factor (PDGF) receptor.
1
M1687 Brivanib alaninate (BMS-582664)
Brivanib alaninate (BMS-582664) is a
novel,orally available and selective
receptor tyrosine kinase inhibitor of
VEGF-R2 and FGF-R1 and -2.
Size:
M1688 Brivanib (BMS-540215)
Brivanib (BMS-540215) is a VEGFR-2
inhibitor with an IC50 value of 25nM.
Size:
M1827 Sorafenib Tosylate (BAY43-9006)
Sorafenib (BAY 43-9006) is an orally active multikinase inhibitor of
tyrosine protein kinases VEGFR/PDGFR and RAF/MEK/ERK with
IC50 values of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant
BRAF.
Size:
HOT
M1840 BGJ398 (NVP-BGJ398)
BGJ398 is a potent and selective FGFR kinase inhibitor with IC50
values of 0.9 nM, 1.4 nM, 1 nM and 60 nM for FGFR1, FGFR2,
FGFR3 and FGFR4, respectively.
Size:
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M1696 Cediranib (AZD2171)
Cediranib (AZD2171) inhibited VEGFR2 and
KDR phosphorylation with IC50s of 0.4 and
0.5 nM, respectively.
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M1805 OSI-930
OSI-930 is a multi-targeted tyrosine kinase
inhibitor of the receptor tyrosine kinases
c-Kit and VEGFR-2 with IC50 values of
9.5 and 10.1 nM.
M1697 Dovitinib (TKI258, CHIR-258)
Dovitinib (TKI258, CHIR-258) is a
small-molecule multitargeted receptor
tyrosine kinase inhibitor.
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M1826 Sunitinib Malate (SU-11248, Sutent)
Sunitinib is a multitargeted tyrosine kinase
inhibitor of VEGFR, PDGFRβ and KIT
inhibitor with Ki values of 2, 9, 17, 8 and
4 nM for VEGFR -1, -2, -3, PDGFRβ and
KIT, respectively.
M1723 Crenolanib (CP-868596)
Crenolanib(CP-868596) is an orally
bioavailable, selective small molecule
inhibitor of PDGFRα and PDGFRβ with
IC50 of 0.9 and 1.8 nM respectively.
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M1841 Lenvatinib (E7080)
Lenvatinib (E7080) is a potent
inhibitor of multiple tyrosine kinases,
including VEGFR3 tyrosine kinase
(IC50=5.2 nM) and VEGFR2 tyrosine
kinase (IC50=4.0 nM).
Size:
M1842 Pazopanib (GW786034)
Pazopanib is an oral angiogenesis
inhibitor of tyrosine kinases, targeting
vascular endothelial growth factor
receptor, platelet-derived growth
factor receptor, and c-Kit.
HOT
HOT

MP1P8II8332KK I nIVnhahitbaiibltaoinrtsiobr dsihydrochloride (PTK787)
Vatalanib is a selective small molecule protein
kinase inhibitor of VEGF receptors 1-3.
Size:
M1918 Amuvatinib (MP470)
Amuvatinib (MP470) is a novel receptor
tyrosine kinase inhibitor that targets
c-KIT and PDGFRα.
Size:
M1956 Apatinib (YN968D1)
Apatinib is a small-molecule multitargeted
tyrosine kinase inhibitor of VEGFR2 with
an IC50 of 2.43 nM.
Size:
M1994 Telatinib (BAY 57-9352)
Telatinib (BAY 57-9352) is an orally
active small-molecule tyrosine kinase
inhibitor of VEGFR2, VEGFR3 and
PDGFRβ with IC50 of 6 nM, 4 nM
and 15 nM, respectively.
Size:
M1995 Ki8751
Ki8751 is a potent, selective inhibitor of
VEGFR-2 tyrosine kinase (IC50=0.9 nM).
M1920 Motesanib Diphosphate (AMG 706)
Motesanib (AMG 706) is a potent ATP
-competitive inhibitor of VEGFR1/2/3,
PDGFR, c-Kit and Ret with IC50 of 2nM,
3 nM, 6 nM, 84 nM, 8 nM and 59 nM,
respectively.
Size:
M1936 E-3810
E-3810 is a novel small molecule
inhibitor with potent and selective
inhibitory activity of the Vascular
Endothelial Growth Factor (VEGF)
receptors 1-3 and of the Fibroblast
Growth Factor (FGF) receptors 1-2.
Size:
M1941 CP 673451
CP 673451 is a potent inhibitor of
platelet-derived growth factor beta
-receptor (PDGFR-beta) with an
IC50 of 1 nM.
Size:
M1944 CP-547632
CP-547632 is a novel VEGFR-2
tyrosine kinase inhibitor with IC50
of 11 nM.
Size:
M1999 DMXAA (Vadimezan, ASA404)
DMXAA (Vadimezan, ASA404) is a tumor
-vascular disrupting agent (tumor-VDA)
and competitive inhibitor of DT-diaphorase
with Ki of 20 μM and IC50 of 62.5 μM,
respectively.
Size:
M2011 PP121
PP121 is a dual inhibitor of tyrosine
and phosphoinositide kinases.
Size:
M2031 SU5416 (Semaxanib)
SU5416 is a novel small molecule multi
-targeted kinase inhibitor of VEGF receptors,
c-kit and FLT3.
Size:
Size:

1
M2074 NVP-BHG712 (BHG712)
NVP-BHG712 is a very potent, selective
inhbitor of the receptor tyrosine kinase
EphB4 (ED50 = 25 nM).
M1705 Erlotinib HCL (Tarceva, CP-358774)
Erlotinib is an inhibitor of human EGFR
tyrosine kinase (IC50 = 2 nM) and
decreases EGFR autophosphorylation
in tumor cells (IC50 = 20 nM).
Size:
M1721 AZD4547
AZD4547 is a potent, selective and orally active pan-FGFR
inhibitor with IC50s of 0.2. 2.5, 1.8 and 165 nM for FGFR1, 2,
3 and 4, respectively.
Size:
M1749 Gefitinib (ZD-1839, Iressa)
Gefitinib (ZD-1839, Iressa) is a novel
potent EGFR tyrosine kinase inhibitor
with an IC50 of 0.40nM.
Size:
Size:
Size:
M2153 TSU-68 (SU6668)
TSU-68 (SU6668) is a protein kinase inhibitor
of PDGF-Rβ, VEGF-R2 and FGF-R1 with IC50
of 0.06, 2.4 and 3.0 μM, respectively.
Size:
M1684 BMS-599626 (AC480)
BMS-599626 (AC480) is an orally bioavailable pan-HER tyrosine
kinase inhibitor with potential antineoplastic activity.
M1699 CP-724714
CP-724714 is a potent and selective orally
active HER-2 tyrosine kinase inhibitor, IC50
= 3 nM.
Size:
M1784 Icotinib (BPI-2009H)
Icotinib (BPI-2009H) is a potent and
novel epidermal growth factor receptor
(EGFR) tyrosine kinase inhibitor (TKI)
with an IC50 of 5 nM.
Size:
M1802 Lapatinib Ditosylate (Tykerb)
Lapatinib Ditosylate is a selective and effective inhibitor of EGFR
kinase (Ki = 3 nM),ErbB-2 kinase (Ki = 13 nM) and ErbB-4 kinase
(Ki = 347 nM).
M2078 SAR131675
SAR131675 is a potent and selective
VEGFR-3 inhibitor with IC50 of 20 nM.
Size:
M2194 SU5402
SU5402 is a potent and selective VEGFR
and FGFR inhibitor with IC50 values of
0.02, 0.03, 0.51 and > 100 μM for
VEGFR2, FGFR1, PDGFRβ and EGFR
respectively.
Size:
EPGI3KF RIn/hHibEitRor2s Inhibitors
M1667 AZD8931
AZD8931 is an equipotent, reversible inhibitor
of Signaling by EGFR, ERBB2 (HER2), and
ERBB3 with IC50 of 4, 3, 4 nM respectively.
Size:
Size:
HOT
HOT
HOT
HOT

MP1P8II5330KK I nIWnhZhib4iib0to0irt2sors
WZ4002 is a novel, selective EGFR kinase
inhibitor against EGFR T790M (mutation of
the gatekeeper T790 residue) with IC50 of
8 nM.
Size:
M1851 WZ8040
WZ8040 is a novel EGFR inhibitor which suppresses the growth of EGFR
-T790M-containing cell lines and inhibits EGFR phosphorylation.
Size:
M1919 Mubritinib (TAK-165)
Mubritinib (TAK-165) is a new potent inhibitor of
human epidermal growth factor receptor 2 (HER2)
tyrosine kinase(IC50 = 6 nM).
Size:
M1943 Canertinib (CI-1033, PD-183805)
Canertinib (CI-1033) is an irreversible
tyrosine-kinase inhibitor with activity
against EGFR (IC50 0.8 nM), HER-2
(IC50 19 nM) and ErbB-4 (IC50 7nM).
HOT
M1869 Dacomitinib (PF-00299804)
Dacomitinib (PF-00299804) is an oral, irreversible,
small molecule inhibitor of human epidermal growth
factor receptor-1, -2, and -4 tyrosine kinases.
Size:
M1875 PD173074
PD173074 is a selective FGFR1 and
FGFR3 inhibitor with IC50 values of 5,
21.5, ~100, 17600 and 19800 nM for
FGFR3, FGFR1, VEGFR2, PDGFR
and c-Src respectively.
Size:
M1904 Pelitinib (EKB-569)
Pelitinib (EKB-569) is an irreversible
EGFR tyrosine kinase inhibitor with
IC50 of 38.5 nM.
Size:
M1913 Neratinib (HKI-272)
Neratinib (HKI-272) is an orally
available, irreversible inhibitor
of Her 2 tyrosine kinase.
Size:
M2021 AG 18 (RG-50810, Tyrphostin 23)
AG-18 is an inhibitor of EGF receptor
kinase with an IC50 value of 35 μM.
Size:
M2117 CNX-2006
CNX-2006 is a novel irreversible
EGFR inhibitor with IC50 value
of <20 nM.
Size:
M2212 CO-1686 (AVL-301, CNX-419)
CO-1686 is a potent, novel inhibitor of
EGFR L858R/T790M kinase with Ki of
21.5 nM and 303.3 nM, respectively.
Size:
Size:
M2255 Genistein (NPI 031L)
Genistein is a highly specific inhibitor
of protein tyrosine kinase (PTK).
Size:
HOT

1
M2312 AG-1478 (Tyrphostin AG-1478)
AG-1478 (Tyrphostin AG-1478) is a selective
EGFR inhibitor with IC50 of 3 nM.
M1766 PF-04217903 (PF-4217903)
PF-04217903(PF-4217903) is a novel ATP-competitive small molecule
inhibitor of c-Met kinases with the IC50 values from 3.1 nM to142 nM.
M1777 SGX523
SGX523 is an exquisitely selective, ATP
competitive inhibitor of the MET receptor
tyrosine kinase with antitumor activity in
vivo.
Size:
M1793 JNJ-38877605
JNJ-38877605 is a small-molecule, ATP
competitive inhibitor of the catalytic activity
of c-Met with an IC50 of 4 nM.
M1682 BMS-777607
BMS-777607 is a selective and potent
small-molecule met kinase inhibitor with
an IC50 of < 0.1μmol/L.
Size:
M1758 Foretinib (XL880, GSK1363089)
Foretinib (XL880, GSK1363089) is a
multi-targeted inhibitor of c-Met and
vascular endothelial growth factor
receptor 2 (VEGFR2) with IC50
value of 0.4 nM for c-MET.
M1765 PF-2341066 (Crizotinib)
PF-2341066 (Crizotinib) is a potent, orally
bioavailable, ATP-competitive small-molecule
inhibitor of c-Met kinase and ALK (anaplastic
lymphoma kinase) with IC50 values to be 4
and 25 nM for C-Met and ALK resepectively.
Size:
M1811 ARQ-197 (Tivantinib)
ARQ-197 (Tivantinib) is a selective
and oral small-molecule inhibitor of
c-Met with a minimal IC50 value of
0.1 μM.
Size:
M1890 SU11274 (PKI-SU11274)
SU11274 is a selective c-Met inhibitor (IC50 = 0.01 μM in vitro).
Size:
M1757 XL-184 (Cabozantinib, BMS-907351)
XL184 is a small molecule inhibits multiple receptor tyrosine kinases,
specifically MET and VEGFR2 with IC50 values of 0.035 and 1.8 nM
for VEGFR2 and Met respectively.
Size:
Size:
M1647 AMG-208
AMG-208 is a potent small molecular inhibitor
c-Met with an IC50 of 9.3 nM.
Size:
M1745 AMG-458
AMG-458 (AMG458) is a potent,
selective inhibitor of c-Met and a
receptor tyrosine kinase that is
often deregulated in cancer.
HOT
HOT
cP-IM3Ke Itn hInibhitiobristors
Size:
Size:
Size:
HOT
HOT
HOT
Size:

MP1P8II9339KK I nIPnhHhiAbii-bt6oi6rts5o7r5s2
PHA-665752 is a selective small molecule c-MET inhibitor (Ki of 4
nM, IC50 of 9 nM).
M1743 X-376
X-376 is a potent and highly specific ALK small molecule tyrosnie
kinase inhibitor.
Size:
M1794 SB431542
SB-431542 is a potent and selective
inhibitor of the transforming growth
factor-β (TGF-β) type I receptor activin
receptor-like kinase ALK5 (IC50=94nM).
Size:
M1901 Golvatinib (E7050)
Golvatinib (E7050) is an orally bioavailable
dual kinase inhibitor of c-Met and VEGFR-2
tyrosine kinases with potential
Size:
M1922 MGCD265
MGCD265 is a novel multitargeted receptor tyrosine kinase (RTK)
inhibitor that targets the mesenchymal epithelial transition (c-Met)
and the vascular endothelial growth factor (VEGF) receptors
(VEGFR1, VEGFR2, and VEGFR3).
Size:
M2080 INCB28060
INCB28060 is a novel inhibitor of c-MET kinase with IC50 of
0.13 nM.
Size:
APIL3KK IInnhhibiibtoitros rs
M1720 AP26113
AP26113 is a highly potent
ALK inhibitor with IC50 of
0.62 nM.
Size:
M1859 ALK5 Inhibitor II (SJN 2511)
ALK5 Inhibitor is a potent and ATP-competitive
inhibitor of the TGF-β type I receptor ALK5.
Size:
M1873 LDN-193189
LDN-193189 is a highly potent small molecule inhibitor of
bone morphogenetic protein (BMP) type I receptors ALK2
and ALK3.
Size:
M1932 GSK1838705A
GSK1838705A is a small-molecule kinase
inhibitor that inhibits IGF-IR and the insulin
receptor with IC50s of 2.0 and 1.6 nmol/L,
respectively.
Size:
Size:
M1942 CH5424802 (AF802)
CH5424802 is a highly selective, orally active and potent ALK
inhibitor with IC50 of 1.9 nM.
Size:

1
M1946 CEP-28122
CEP-28122 is a highly potent and selective orally active ALK ihnibitor.
M1821 OSI-906 (Linsitinib)
OSI-906 (Linsitinib) is a potent, selective
dual ATP-competitive tyrosine kinase
inhibitor of insulin-like growth factor-1
receptor (IGF-1R) and insulin receptor
(IR) with IC50 values of 35 nM and 75
nM respectively.
M1777 SGX523
SGX523 is an exquisitely selective, ATP
competitive inhibitor of the MET receptor
tyrosine kinase with antitumor activity in
vivo.
Size:
M1957 BMS-536924
BMS-536924 is an ATP-competitive
IGF-IR and IR inhibitor with IC50 of
100 nM and 73 nM respectively.
M2075 LDK378
LDK378 is a highly selective, orally
bioavailable ALK inhibitor with IC50
of 0.15 nM.
Size:
M1717 GSK1904529A
GSK1904529A selectively inhibits IGF-IR and IR with IC50s of 27
and 25 nmol/L, respectively.
M1792 XL228
XL228 is a potent multikinase small-molecule
inhibitor of insulin-like growth factor type 1
receptor (IGF1R).
Size:
M2025 PQ401
PQ401 is an insulin growth factor-1
receptor (IGF-1R) inhibitor.
Size:
M2192 BMS-754807
BMS-754807 is an ATP-competitive dual
kinase inhibitor of IGF-1R and IR with IC50s
of 1.8 nM and 1.7 nM, respectively..
Size:
Size:
M1950 ASP3026
ASP3026 is a novel and selective
inhibitor for the ALK kinase.
Size:
M2109 AZD3463
AZD3463 is a novel ALK/IGF1R inhibitor
with IC50 value of 22 nM.
Size:
Size:
Size:
Size:
IPGI3FK- 1InRh iIbnithoribs itors

Angiogenesis
Angiogenesis
FPLI3TK3 PI3K Inhibitors
In Ihnihbiitboritsors
SPrI3cK-b Inchri-bAitobrls Inhibitors
M1648 AP24534 (Ponatinib)
Ponatinib (AP24534) is a novel
potent, available small molecule
multitargeted kinase inhibitor of
BCR-ABL, PDGFRα,c-Src, c-Kit,
FGFR and VEGFR.
M1641 AC220 (Quizartinib)
AC220 (Quizartinib) is a uniquely potent
and selective FLT3 inhibitor.
Size:
M1815 KW-2449
KW-2449 is a novel multitargeted
kinase inhibitor of FLT3, ABL and
Aurora kinase with IC50 values of
6.6 nM, 14 nM and 48 nM.
Size:
M1828 Tandutinib (MLN518, CT53518)
Tandutinib (MLN518), previously known
as CT53518, is an orally active multitargeted
tyrosine kinase inhibitor of FLT3, PDGFR
and c-Kit.
Size:
HPII3FK I Innhhiibbiitotorsrs
M1726 FG-4592 (ASP1517)
FG-4592 (ASP1517) is a novel
Hypoxia Inducible Factor Prolyl
Hydroxylase inhibitor.
HOT
Size:
M1992 2-Methoxyestradiol (2ME2)
2-Methoxyestradiol is a natural
metabolite of estradiol acts via
an estrogen receptor-independent
mechanism.
Size:
M1659 Saracatinib (AZD0530)
Saracatinib (AZD0530) is an orally active
small molecule Src inhibitor.
Size:
M1685 Bosutinib (SKI-606)
Bosutinib (SKI-606) is a novel
Bcr-Abl inhibitor with IC50 values
of 0.1 to 0.3 umol/L.
Size:
M1701 Dasatinib (BMS-354825)
Dasatinib is a small molecule
inhibitor of both the SRC and
BCR/ABL tyrosine kinases.
Size:
M1712 FTY720 (Fingolimod)
FTY720 (Fingolimod) is a sphingosine-1-phosphate receptor
1 receptor.
Size:
Size:
M1799 Imatinib Mesylate (Gleevec, Glivec)
Imatinib Mesylate is a Bcr-Abl tyrosine kinase inhibitor, with
IC50 values of 2.9 and 3.9 μM for the inhibition of T-cell
proliferation stimulated by PHA and DCs respectively.
Size:

PI3K/Akt/mTORAngiogenesis
1
M1825 PCI-32765 (Ibrutinib)
PCI-32765 (Ibrutinib) is a potent, selective
and orally bioavailable irreversible inhibitor
of BTK with IC50 value of 0.46 nM.
Size:
10mg 50mg 200mg >1000mg Inquiry Size:
M1991 Bafetinib (INNO-406, NS-187)
Bafetinib (NS-187, INNO-406) is a novel second-generation dual
Bcr-Abl/Lyn tyrosine kinase inhibitor.
Size:
Size:
FPAI3KK IInnhhibiibtoitros rs
Angiogenesis
M1847 Fostamatinib disodium(R788, R935788)
Fostamatinib disodium (R788, R-935788) is a
potent, ATP-competitive and selective Syk
inhibitor with IC50 of 41 nM.
M2331 PP2 (AG 1879)
PP2 is a selective inhibitor of Src-family tyrosine
kinases with >10,000-fold selectivity over ZAP70
and JAK2.
M1990 R788 (Fostamatinib)
R788 (Fostamatinib) is a spleen tyrosine
kinase (Syk) inhibitor with IC50 of 41 nM.
M2063 P505-15 hydrochloride (PRT062607)
P505-15 (PRT062607) is a novel, highly
selective inhibitor of Syk with IC50 value
of 1-2 nM.
Size:
M1912 Nilotinib (AMN107)
Nilotinib (AMN107) is a small molecule
Bcr-Abl kinase inhibitor with IC50 less
than 30 nM.
Size:
M2313 KX2-391
KX2-391 (KX01) is a highly selective non
ATP-competitive Src inhibitor with GI50 of
9-60 nM in cancer cell lines .
Size:
Size:
Size:
SPyI3kK IInnhhiibbitiotrosrs
M1767 R-406
R406 is an orally bioavailable and selective inhibitor of spleen
tyrosine kinase (Syk) with the IC50 of 41nM and Ki value of 30nM.
Size:
M2301 NVP-TAE226 (TAE226)
NVP-TAE226, a potent dual FAK
/IGF-1R, inhibiting FAK and IGF-1R
with IC50 of 5.5 nM and 0.14 μM,
respectively.
Size:
M2302 PF-562271
PF-562271 is a potent, ATP-competitive, reversible inhibitor of
FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively.
Size:
M2113 AVL-292 (CC-292)
AVL-292 is an oral, potent and selective
small molecule covalent inhibitor of Btk
(IC50 < 0.5 nM).
HOT
HOT
NEW
NEW

Apoptosis
Apoptosis
BPIc3lK-PI3K 2 Inhibitors
In Ihnibhiitboristors
pP5I33K IInnhhiibbitiotorsrs
M2027 Tenovin-1
Tenovin-1 is a small molecule
activator of p53 transcriptional
activity.
M1637 ABT-263 (Navitoclax)
ABT-263 (Navitoclax) is a potent, orally bioavailable inhibitor of
the antiapoptotic Bcl-2 family members Bcl-2,Bcl-x (L),and Bcl-w.
Size:
M1638 ABT-737
ABT-737 is a potent and selective
inhibitor of B-cell lymphoma-2
family proteins, in small cell lung
cancer.
Size:
M1860 AT-101
AT-101(R-(-)-gossypol acetic acid)
is a pan small molecule inhibitor
of Bcl-2, Bcl-xL, and Mcl-1.
Size:
M2017 ABT-199 (GDC-0199)
ABT-199 is a highly potent, orally BCL-2 inhibitor.
Size:
M2314 TW-37
TW-37 is a novel nonpeptide
inhibitor to recombinant Bcl-2,
Bcl-xL and Mcl-1 with Ki of
0.29μM, 1.11μM and 0.26μM,
respectively.
Size:
M2036 Pifithrin-α
Pifithrin-α is an inactivator of p53 that
blocks p53-dependent transcriptional
activation and apoptosis.
Size:
M2068 JNJ-26854165 (Serdemetan)
JNJ-26854165(Serdemetan) is a novel
activator of p53 capable of inducing
apoptosis in cancer cell lines.
Size:
TPNI3FK- Ianlhpibhitao rIsnhibitors
M1962 Lenalidomide (Revlimid, CC-5013)
Lenalidomide is a thalidomide analog
known to display TNF-α secretion
inhibition and possesses immuno
-modulatory properties.
Size:
M1976 Pomalidomide (Actimid, CC-4047)
Pomalidomide is a second generation
immunomodulator,TNF-α inhibitor with
IC50 of 13 nM.spectively.
Size:
M2225 Thalidomide (Thalomid)
Thalidomide is a selective inhibitor
of tumor necrosis factor α (TNF-α)
synthesis.
Size:
Size:

PI3K/Akt/mTORApoptosis
1
M2315 Necrostatin-1
Necrostatin-1 is a specific RIP1 inhibitor
and inhibits TNF-α-induced necroptosis
with EC50 of 490 nM.
Size:
M1867 PAC-1
PAC-1 is a procaspase-activating
compound;activates procaspase-3
to produce caspase-3 (EC50 =
0.22 μM).
Size:
Size:
FPAI3KK IInnhhibiibtoitros rs
Apoptosis
M1847 Fostamatinib disodium(R788, R935788)
Fostamatinib disodium (R788, R-935788) is a
potent, ATP-competitive and selective Syk
M2331 PP2 (AG 1879)
PP2 is a selective inhibitor of Src-family tyrosine
kinases with >10,000-fold selectivity over ZAP70
and JAK2.
M1990 R788 (Fostamatinib)
R788 (Fostamatinib) is a spleen tyrosine
kinase (Syk) inhibitor with IC50 of 41 nM.
M2063 P505-15 hydrochloride (PRT062607)
P505-15 (PRT062607) is a novel, highly
selective inhibitor of Syk with IC50 value
of 1-2 nM.
Size:
M2313 KX2-391
KX2-391 (KX01) is a highly selective non
ATP-competitive Src inhibitor with GI50 of
9-60 nM in cancer cell lines .
Size:
Size:
Size:
SPyI3kK IInnhhiibbitiotrosrs
M1767 R-406
R406 is an orally bioavailable and selective inhibitor of spleen
tyrosine kinase (Syk) with the IC50 of 41nM and Ki value of 30nM.
Size:
M2301 NVP-TAE226 (TAE226)
NVP-TAE226, a potent dual FAK
/IGF-1R, inhibiting FAK and IGF-1R
with IC50 of 5.5 nM and 0.14 μM,
respectively.
Size:
M2302 PF-562271
PF-562271 is a potent, ATP-competitive, reversible inhibitor of
FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively.
Size:
M2113 AVL-292 (CC-292)
HOT
AVL-292 is an oral, potent and selective
small molecule covalent inhibitor of Btk
(IC50 < 0.5 nM).
NEW
NEW
CPIa3sKp Inahsiebi tIonrhsibitors
MMddmm22it oInrshibitors

JAK/STAT
JAK/STAT
PI3K Inhibitors M1787 INCB18424 (Ruxolitinib)
INCB18424 is a potent inhibitor of both
JAK1 and JAK2 with selectivity versus
JAK3 and TYK2 (IC50 values of 2.7,
4.5, 332, and 19 nM, respectively, in
biochemical assays).
JPAI3KK IInnhhibibitoitrosrs
M1646 AG490 (Tyrphostin AG490)
AG490 (Tyrphostin AG490) is a
selective inhibitor of EGF receptor
tyrosine kinase (IC50 values are 2
and 13.5 μM for EGFR and ErbB2
respectively).
Size:
M1660 AZ 960
AZ 960 is a novel and specific
inhibitor of the JAK2 kinase with
a Ki of 0.45nM in vitro.
Size:
M2125 WP1066
WP1066 is a potent, novel inhibitor of
JAK2 and STAT3 with IC50 of 2.3 μM
and 2.43 μM in HEL cells.
Size:
M1700 CYT387 (CYT 11387)
CYT387 is a small-molecule, ATP
-competitive JAK1/JAK2 inhibitor
with IC50 of 11 and 18 nM
respectively.
Size:
HOT
M1733 TG101348
TG101348 is a selective small-molecule
Janus kinase 2(JAK2) inhibitor with IC50
of 3 nM.
Size:
HOT
M1804 NVP-BSK805 HCL(BSK805)
NVP-BSK805 dihydrochloride is
a potent and selective quinoxaline
JAK2 inhibitor with IC50 values
of 0.48, 0.56 and 0.58 nM for JAK2
JH1, FL JAK V617F and FL JAK2
wt respectively.
Size:
M1820 Tofacitinib (CP-690550, Tasocitinib)
Tofacitinib (Tasocitinib, CP-690550) is
a novel Janus Kinase 3 (JAK-3) kinase
inhibitor with an IC50 value estimated
at 0.2 μM.
Size:
HOT
M1887 TG101209
TG101209 is a novel small molecule, ATP-competitive JAK2
-selective kinase inhibitor (IC50 = 6 nM).
Size:
M2039 Baricitinib (INCB28050, LY3009104)
Baricitinib (INCB28050) is an oral JAK1
and JAK2 inhibitor with IC50 of 5.9 nM
and 5.7 nM, respectively.
Size:
M2044 AZD1480
AZD1480 is a novel small-molecule
inhibitor of JAK1/2 with IC50 of 1.3
nM and 0.26 nM, respectively.
Size:
M1754 WP1130
WP1130 is a small molecular
deubiquitinase (DUB) inhibitor
and suppresses JAK-Stat
signaling pathway.
Size:
Size:

PI3K/Akt/mTORJAK/STAT
1
M2064 CEP-33779
CEP-33779 is a novel, orally active,
selective JAK2 inhibitor with IC50 of
1.8 nM.
PPiI3mK IInnhhibibitiotrosrs
M1779 SGI-1776
SGI-1776 is novel small molecule
inhibitor of PIM kinase activity with
IC50 of 7 ± 1.8, 363 ± 27.6 and
69 ± 9.2 nM for Pim-1, Pim-2,
and Pim-3, respectively.
Size:
Size:
MAPK
JAK/STAT
M2028 Fludarabine
Fludarabine is a STAT1 activation
inhibitor and a DNA synthesis inhibitor.
M1661 AZD6244 (Selumetinib, ARRY-142886)
AZD6244(ARRY-142886, Selumetinib)
is a potent MEK 1/2 inhibitor with GI50
values ranging from 14 to 50 nM.
M1662 AZD8330 (ARRY-424704, ARRY-704)
AZD8330 (ARRY-424704) is a novel,
highly efficacious, uncompetitive MEK
inhibitor with an IC50 of 7 nM.
Size:
Size:
Size:
M1782 NSC 74859 (S3I-201)
NSC74859 (S3I-201) is a STAT3 inhibitor
and is effective in hepatocellular cancers
with disrupted TGF-beta signaling.
Size:
Size:
Size:
Size:
M2055 Niclosamide (Niclocide)
Niclosamide is an inhibitor of STAT3
with an IC50 value of 0.25 μM.
Size:
M1690 CI-1040 (PD184352)
CI-1040 (PD184352) is a targeted
signal transduction inhibitor of MEK
with a ki value of 300nM in vitro.
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M1744 ARRY-162 (MEK-162, ARRY-438162)
ARRY-162 is a selective,potent
inhibitor of MEK and cellular pERK
with IC50 of 12 nM and 11nM,
respectively.
Size:
M1750 TAK-733
TAK-733 is a potent and selective
MEK allosteric site inhibitor with
IC50 of 3.2nM for the treatment
of cancer.
SMTdAmT2i tIonrshibitors
M2239 SB1317 (TG02)
SB1317 (TG02) is a novel small molecule
potent CDK/JAK2/FLT3 inhibitor.
MPIE3KK I nInhihbiibtoirtsors
M1652 AS703026 (MSC1936369B,Pimasertib)
AS703026 is a novel selective MEK1/2
inhibitor, and induces pleiotropic anti
-myeloma activity in vitro and in vivo.
HOT
HOT

MAPK
MAPK
M1759 GSK1120212 (JTP-74057, GSK212)
GSK1120212 (JTP-74057) is a highly
potent and selective MEK inhibitor with
IC50 values to be 0.7 and 0.9 nM for
MEK1 and MEK2 respectively and with
long circulating half-life.
PI3K Inhibitors M2316 BIX02189
BIX02189 is a selective inhibitor
of MEK5 with IC50 of 1.5 nM.
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M1763 PD-0325901 (PD325901)
PD-0325901 is a highly potent
and selective MEK inhibitor with
an IC50 in C26 cells of 0.33nM.
Size:
HOT
M1822 PD98059
PD98059 is a potent and selective inhibitor
of mitogen-activated protein kinase kinase
(MKK / MEK) with IC50 value of 2-7 μM.
Size:
M1905 PD318088
PD318088 is a non-ATP competitive
allosteric MEK1/2 inhibitor.
Size:
HOT
M1977 U0126
U0126 is a potent and highly selective
non-competitive inhibitor of MAPK/ERK
kinase with IC50 of 72 nM for MEK1
and 58 nM for MEK2.
Size:
pP3I38K MInAhiPbiKto rIsnhibitors
M1675 BIRB796 (Doramapimod)
BIRB 796 (Doramapimod) is a protein
kinase inhibitor of p38 MAPK with Kd
of 100pM.
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M1781 SB203580 (RWJ 64809, PB 203580)
SB203580 inhibits the IL-2-induced
proliferation of primary human T cells,
murine CT6 T cells, or BAF F7 B cells
with an IC50 of 3-5 μM.
Size:
HOT
M2084 SCH772984
SCH772984 is a novel and selective inhibitor of ERK1/2 with
IC50 of 4 nM and 1 nM, respectively.
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M2177 BIX02188
BIX02188 is a novel specific inhibitor
of MEK5 which inhibits catalytic function
of purified, MEK5 enzyme.
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M2062 SB 202190
SB 202190 is a highly selective,
and cell permeable inhibitor of p38
MAP kinase with IC50 values of 50
and 100nM inhibiting p38α and p38β,
respectively.
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M2136 PH-797804
PH-797804 is a highly selective
and potent inhibitor of p38 MAP
kinase with IC50 of 26 nM.
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M2317 VX-702
VX-702 is a highly selective inhibitor
of p38 MAPKα with IC50 of 4-20 nM.
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PI3K/Akt/mTORMAPK
1
M2318 LY2228820
LY2228820 is a novel and potent
inhibitor of p38 MAPK with IC50
of 7 nM.
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M1714 GDC-0879
GDC-0879 is a potent and selective
B-Raf kinase inhibitor with an EC50
of 0.75 μM.
MAPK
M1863 RAF265 (CHIR-265)
RAF265 is a novel, orally bioavailable dual inhibitor of RAF kinase
and VEGFR2.
M1988 Dabrafenib (GSK2118436)
Dabrafenib (free base) (GSK2118436A)
is a V600 mutant BRAF-specific inhibitor.
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M1761 PLX4032 (Vemurafenib, RG7204)
PLX4032 (Vemurafenib, RG7204, RO5185426 and Zelboraf) is
a highly selective B-Raf enzyme inhibitor with an IC50 of 44 nM
against V600E-mutant BRAF.
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M1783 SB590885
SB590885 is another selective small
molecule inhibitor of the B-Raf kinase
and Ki app values are 0.16 and 1.72nM
for B-Raf and c-Raf respectively.
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M2045 CEP-32496
CEP-32496 is a potent orally
active BRAF inhibitor with IC50
of 14 nM.
Size:
M2090 MLN2480 (BIIB-024)
MLN2480 (BIIB-024) is an oral,
selective pan-Raf kinase inhibitor.
Size:
M2235 TAK-632
TAK-632 is a potent and selective pan-RAF inhibitor.
RPIa3fK I Innhhiibbiitotorsrs
Size:
M1818 ZM 336372
ZM 336372 is a potent, selective ATP-competitive inhibitor
of c-Raf in vitro (IC50 = 70 nM for inhibition of human c-Raf).
M1855 Dabrafenib Mesylate(GSK-2118436B)
Dabrafenib (GSK2118436) is a selective,
orally bioavailable inhibitor of Mutant B-raf
(BRAF) protein kinase with potential
M1774 PLX4720
PLX4720 is a selective BRAFV600E inhibitor
with the IC50 values of 160nM and 130 nM
for B-Raf and BRK respectively.
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Cytoskeletal Signaling
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PI3K Inhibitors
M1679 BIIB021 (CNF2024)
BIIB021 (CNF2024) is an orally available
synthetic non-ansamycin Hsp90 inhibitor
with ki value of 1.7nM.
M2319 AZ628
AZ628 is a potent inhibitor for wild
-type CRAF and BRAF V600E with
IC50 of 29nM and 34nM,respectively.
M1741 Ganetespib (STA-9090)
Ganetespib (STA-9090) is a potent
synthetic small molecule inhibitor of
Hsp90 with potential antineoplastic
activity.
M2013 JNK-IN-8
JNK-IN-8 is a selective JNK inhibitor that inhibits phosphorylation
of c-Jun.
M1725 CUDC-305
CUDC-305 is a heat shock protein 90
inhibitor of the novel imidazopyridine
class.
M2076 SP600125
SP600125 is a novel and selective inhibitor
of c-Jun N-terminal kinase (JNK), inhibited
phosphorylation of c-Jun with an IC50 of 5
-10 microM.
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M1798 NVP-HSP990 (HSP990)
NVP-HSP990 is an orally bioavailable
inhibitor of human heat-shock protein
90 with potential antineoplastic activity.
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HPIS3KP 9In0h iIbnithoirbsitors
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M1762 AUY922 (NVP-AUY922)
AUY922 (NVP-AUY922) is a small
molecule Heat Shock Protein 90
(HSP90) inhibitor with IC50 values
of 13 and 21 nM for HSP90α and
HSP90β respectively.
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M1908 NVP-BEP800 (VER-82576)
NVP-BEP800 is a novel, fully synthetic,
orally bioavailable inhibitor of Hsp90β
with an IC50 of 58 nM.
JPNI3KK IInnhhibibitoitrosrs
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PI3K/Akt/mTORCytoskeletal Signaling
1
M1949 AT13387
AT13387 is a novel, high-affinity
heat-shock protein 90 (HSP90)
inhibitor with IC50 of 18 nM in
A375 cells.
M2003 PF-04929113 (SNX-5422)
PF-04929113 (SNX-5422) is
a potent and selective Hsp90
inhibitor with Kd of 41 nM.
M1970 Paclitaxel (Taxol)
Paclitaxel is a mitotic inhibitor with
IC50 of 0.1 pM in human endothelial
cells.
M2083 Elesclomol (STA-4783)
Elesclomol (STA-4783) is a small-molecule investigational agent
that selectively induces apoptosis in cancer cells by increasing
oxidative stress.
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M1892 Vincristine sulfate (leurocristine)
Vincristine(leurocristine) is a mitotic
inhibitor used in cancer chemotherapy.
M1940 Docetaxel (Taxotere)
Docetaxel (Taxotere), a semi-synthetic
analog of paclitaxel, is a promoter of
microtubule polymerization leading to
cell cycle arrest at G2/M, apoptosis
and cytotoxicity.
Size:
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M2070 XL888
XL888 is a novel small-molecule inhibitor
of HSP90 with IC50 of 24nM.
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M2320 17-AAG (Tanespimycin)
17-AAG (Tanespimycin) is a potent
HSP90 inhibitor with IC50of 5 nM.
M1952 ASC-J9
ASC-J9 is an AR degradation enhancer.
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M2274 Fosbretabulin disodium
Fosbretabulin disodium is a microtubule
-targeting agent that binds β-tubulin with
Kd of 0.4 μM.
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M2321 17-DMAG HCL (Alvespimycin)
17-DMAG (Alvespimycin) is a potent
HSP90 inhibitor with IC50 of 62 nM.
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MPIi3cKr oInthuibbiutolres Inhibitors
M1642 ABT-751
ABT-751 is an orally bioavailable tubulin
inhibitor with IC50 of about 1.5 and 3.4μM
in neuroblastoma and non-neuroblastoma
cell lines, respectively.
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KPIi3nKe Isnihnib Iintohrsibitors
PI3K Inhibitors
M1796 XAV939
XAV939 is a potent, cell-permeable
small molecule inhibitor of the Wnt/β
catenin pathway to TNKS1 and TNKS2
with IC50 values of 11 and 4 nM
respectively.
M2237 IWP-2
IWP-2 is an inhibitor of Wnt production
that impairs Wnt pathway activity in vitro
with an IC50 value of 27 nM.
M2042 Cilengitide (EMD121974,NSC707544)
Cilengitide (EMD 121974, NSC 707544) is a
selective inhibitor of αvβ3 integrin and αvβ5
integrin with IC50 of 1 nM and 140 nM,
respectively.
M2008 ICG-001
ICG-001 is a novel small molecule
inhibitor of TCF/beta-catenin
-mediated transcription.
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WPI3nKt/ bInehtibai-tocrastenin Inhibitors
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IKnitneegsirni nIn Ihnibhitiobristors
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M1786 Ispinesib (SB-715992, CK0238273)
Ispinesib (SB 715992) is the first potent,
highly specific small-molecule inhibitor of
kinesin spindle protein (KSP) with an IC50
of 4.1 nM.
M1983 SB-743921
SB-743921 is a highly potent and active
KSP inhibitor with a Ki of 0.1 nM for KSP
(Eg5).
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M2128 AZ3146
AZ3146 is a potent and selective monopolar spindle 1(Mps1)
kinase inhibitor with IC50 of 35 nM.
Size:
M2171 GSK923295
GSK923295 is an allosteric inhibitor of CENP-E with Ki value
of 3.2 nM.
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HOT

PI3K/Akt/mTORCell Cycle
M1655 AT9283
AT9283 is a potent inhibitor of several protein kinases, including
Aurora A, Aurora B, Janus kinase 2 (JAK2), JAK3, and ABL.
M2103 CCT137690
CCT137690 is a potent inhibitor of
Aurora kinases with IC50 values of
15, 19, 25 nM at Aurora A, Aurora
C and Aurora B respectively.
M1691 CCT-129202
CCT129202 is an Aurora kinase inhibitor
with IC50 of 0.042 ± 0.022, 0.198 ± 0.05,
and 0.227 ± 0.064 μmol/L for Aurora A,
Aurora B, and Aurora C, respectively.
26 info@abmole.com www.abmole.com ● Shop Online 1
Cell Cycle
M1877 ZM447439
ZM447439 is the first Aurora family kinase
inhibitor with IC50 of 50 nM for Aurora B
kinase.
M1663 AZD1152-HQPA (Barasertib)
AZD1152-HQPA (Barasertib) is a highly potent and selective
inhibitor of Aurora with Ki values of 0.36 and 1369 nM for Aurora
B and Aurora A respectively.
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M1694 CYC116
CYC116 is a potent, small molecule inhibitor
of Aurora A, B and C with IC50 value of 44,
19 and 65 nM respectively.
M1881 Tozasertib (VX-680, MK-0457)
Tozasertib(VX-680,MK-0457) is a
potent and selective pan-Aurora
kinase inhibitor active against all
Bcr/Abl proteins.
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M2127 Hesperadin
Hesperadin is an ATP-competitive
inhibitor of Aurora B kinase with
IC50 of 250 nM.
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M1706 ENMD-2076
ENMD-2076 is an orally-active, Aurora
A/angiogenic kinase inhibitor.
M1752 MLN8237 (Alisertib)
MLN8237 (Alisertib) is a second-generation,
orally bioavailable, highly selective Aurora
kinase A inhibitor with IC50 of 61 nM.
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APIu3rKo Irnah iKbiitonrasse Inhibitors
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M1751 MLN8054
MLN8054 is an orally bioavailable,
highly selective small molecule
inhibitor of Aurora with IC50s of
0.004uM and 0.172uM. for Aurora
A and Aurora B.
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M1769 PHA-739358 (Danusertib)
PHA-739358 (Danusertib) is a small
molecule with low nanomolar activity
against all aurora kinases (AKs) with
IC50 value of 13 nM for aurora-A and
79 nM for aurora-B respectively.
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Cell Cycle
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CPID3KK InInhhibiibtoirtsors
M1653 AT7519
AT7519 is a novel small molecule multi
-cyclin-dependent (CDK) kinase inhibitor.
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Cell Cycle
PI3K Inhibitors
M1796 PF-477736 (PF-0044736)
PF-477736 is a selective checkpoint
kinase 1(Chk1) inhibitor with Ki values
of 0.49 nM and 47 nM for CHK1 and
CHK2 respectively.
M1806 PD 0332991 (PD0332991, Palbociclib)
PD 0332991 is a highly specific
inhibitor of Cdk4(IC50, 0.011
micromol/L) and Cdk6 (IC50,
0.016 micromol/L).
M2154 TAK-901
TAK-901 is a novel small-molecule inhibitor
of Aurora A and Aurora B with IC50 of 21nM
and 15 nM.
M1800 JNJ-7706621
JNJ-7706621 is a dual cell cycle
inhibitor with activity against cyclin
-dependent kinases (CDK1, 2, 3,
6) with an IC50 of 3-175 nM and
Aurora kinases (A and B) with an
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M2169 AMG 900
AMG900 is a potent and selective,
orally available small molecule
aurora kinase inhibitor.
M2188 Reversine
Reversine is a novel small molecule
ATP-competitive Aurora kinase
inhibitor with IC50 of 98.5 nM for
Aurora B.
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M1710 Flavopiridol (Alvocidib, HMR-1275)
Flavopiridol (Alvocidib) is a pan-cdk
inhibitor of CDKs 1, 2 and 4 in cell-free
assays (IC50 in the region of
100 nM).
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M1740 R547
R547 is a potent and selective
ATP-competitive CDK inhibitor.
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M1807 SCH727965 (Dinaciclib)
SCH727965 (Dinaciclib) is a potent and
selective CDK inhibitor with IC50 values
of 1, 1, 3 and 4 nM for CDK2,CDK5,CDK
1 and CDK9, respectively.
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M1810 AZD5438
AZD5438 is a novel, orally bioavailable
inhibitor of cyclin-dependent kinase(CDK)
1, 2 and 9 (IC50 values are 16, 6 and 20
nM respectively).
M1974 Roscovitine (Seliciclib, CYC202)
Roscovitine is a potent and selective
inhibitor of the cyclin-dependent kinases
cdc2, cdk2 and cdk5.
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PI3K/Akt/mTORCell Cycle
M2065 SNS-032 (BMS-387032)
SNS-032 (BMS-387032) is a potent and selective
inhibitor of CDK 9, 2 and 7 with IC50 values of 4,
38 and 62 nM respectively.
M2324 LY2603618 (IC-83)
LY2603618 (IC-83) is a selective Chk1
inhibitor with potential anti-tumor activity.
M2218 LEE011
LEE011 is a novel, orally available,
potent and selective CDK4/6 inhibitor.
Cell Cycle
M1716 Gemcitabine HCL(Gemzar, LY-188011)
Gemcitabine (Gemzar, LY188011)
inhibits DNA synthesis with an IC50
of 0.06 μM.
M2112 LY2835219
LY2835219 is an orally available inhibitor of CDK4 and CDK6
with IC50 of 2 nM and 10 nM, respectively.
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M2322 PHA-767491 (CAY10572,PHA767491)
PHA-767491 is a potent ATP-competitive
dual Cdc7/CDK9 inhibitor with IC50 of 10
nM and 34 nM, respectively.
M1996 SCH 900776
SCH 900776 is a highly potent and
functionally selective CHK1 inhibitor
with IC50 of 3 nM.
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M2325 CHIR-124
CHIR-124 is a novel and potent Chk1
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M2323 BMS265246
BMS265246 is a potent and selective CDK
inhibitor for CDK1/cyclin B and CDK2/cyclin
E with IC50 of 6 nM and 9 nM, respectively.
M1676 BIBR1532
BIBR1532 is a potent and selective
telomerase inhibitorwith IC50 of 93nM.
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M1665 AZD7762
AZD7762 is a potent ATP-competitive
checkpoint kinase inhibitor with an IC50
of 5 and <10 nM for CHK1 and CHK2
respectively.
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M1698 Clofarabine (Clolar, Evoltra)
Clofarabine inhibits the enzymatic
activities of ribonucleotide reductase
(IC50 = 65 nM) and DNA polymerase.
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CPIh3eKc Inkhpiboiitnorts Inhibitors
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Cell Cycle
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M2148 RKI-1447
RKI-1447 is a potent small molecule inhibitor of ROCK1 and
ROCK2 with IC50 of 14 nM and 6 nM, respectively.
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PPLI3KK IInnhhibibitoitrosrs
M1678 BI 6727 (Volasertib)
BI6727(Volasertib) is a small highly potent Polo-like kinase inhibitor
(Plk1) with an IC50 of 0 .87 nM.
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M2211 Rigosertib (ON-01910)
Rigosertib is a dual non-ATP inhibitor of polo-like kinase 1
(Plk1) and phosphoinositide 3-kinase pathways (PI3K).
Size:
RPIO3KC IKnh Iinbihtoibrsitors
M1817 Y-27632 dihydrochloride
Y-27632 is a potent, selective inhibitor
of Rho-associated protein kinases with
IC50 values of 140-220 nM for ROCK1
and ROCK2.
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Cell Cycle
PI3K Inhibitors
M1856 Thiazovivin
Thiazovivin is a selective small molecule
Rho-associated kinase (ROCK) inhibitor
which significantly improves (200-fold)
the efficiency of iPSC generation from
human fibroblasts.
M2143 MK-1775 (Seliciclib, CYC202)
MK-1775 is a potent and selective
small molecule Wee1 kinase inhibitor
with IC50 of 5.2 nM.
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M1672 BI 2536
BI 2536 is a novel, highly selective,
potent inhibitor of Polo-like kinase
1 (Plk1) with an IC50 of 0.83 nM.
M1719 GSK461364
GSK461364 is a potent and selective
small molecule inhibitor of Polo-like
kinase 1 (PLK1) with a Ki of 2.2 nM.
M1872 Fasudil hydrochloride (HA-1077)
Fasudil hydrochloride is a potent Rho
-associated kinase inhibitor with IC50
of 10.7 μM.
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WPI3eKe 1In hInibhitiobristors
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PI3K/Akt/mTORTGF-beta/Smad
M2016 LY364947 (HTS 466284)
LY364947 is a selective small molecule
inhibitor of the TGFβ type I receptor
kinase with IC50 of 59 nM.
TGF-beta/Smad
M1704 Enzastaurin (LY317615)
Enzastaurin inhibits PKCβ,PKCα,PKCγ
and PKCε with IC50's of 0.006, 0.039,
0.083 and 0.110 μM, respectively.
M2000 GW788388
GW788388 is a potent selective
inhibitor of TGF-beta type I receptor
and ALK5 with IC50 values of
0.093 and 0.018 μM.
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M2081 LY2109761
LY2109761 is a novel TGF-β receptor
type I and type II dual inhibitor.
M2019 Go 6983 (Goe 6983)
Go 6983 is a fast acting, lipid soluble,
broad spectrum protein kinase C inhibitor.
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M2066 Staurosporine (AM-2282)
Staurosporine (AM-2282) is a potent
PKC inhibitor with IC50 of 2.7 nM.
M2108 SB-525334
SB-525334 is a potent activin receptor-like
kinase (ALK5)/ type I TGFβ-receptor kinase
M2328 Pirfenidone
Pirfenidone inhibits TGF-β bioactivity by
affecting TGF-β2 mRNA expression and
processing of pro-TGF-β in CCL-64 cells.
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M2149 Astragaloside IV (Astragaloside A)
Astragaloside IV is a novel regulator of HIF
-1α and angiogenesis through the PI3K/Akt
pathway in HUVECs.
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TPGI3KF -Ibnheitbait oInrshibitors
M1980 LY2157299
LY2157299 is a novel clinically relevant
TBRI (ALK5 kinase) inhibitor with IC50
of 56 nM.
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PPKI3KC InInhhibiibtoirtsors
M1861 CX-4945 (Silmitasertib)
CX-4945 (Silmitasertib) is a potent
small molecule protein kinase inhibitor
that selectively binds to and inhibits
the enzyme casein kinase II (CK2).
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M2208 Sotrastaurin (AEB071)
Sotrastaurin is an orally available pan
-protein kinase C(PKC) inhibitor with
potential immunosuppressive and anti-neoplastic
activities.
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DNA Damage
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M1747 LAQ824 (NVP-LAQ824)
LAQ824 (NVP-LAQ824) is a potent novel
histone deacetylase (HDAC) inhibitor with
an IC50 of 0.032 μM.
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HPID3KA CInh Iinbhitoibrsitors
M1693 CUDC-101 (Curis)
CUDC-101 is a potent multitargeted HDAC,
EGFR and HER2 inhibitor with IC50 of 4.4,
2.4, and 15.7 nM, respectively.
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M1722 CHR-3996
CHR-3996 is an orally bioavailable,
second-generation hydroxamic acid
based inhibitor of HDAC with potential
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M1730 ITF2357 (Givinostat, Gavinostat)
ITF2357 (Givinostat, Gavinostat) is a histone deacetylase
inhibitor. The IC50 values for maize HDAC preparations HD2,
HD-1B and HD-1A are 10, 7.5 and 16 nM respectively.
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HOT
DNA Damage
PI3K Inhibitors
M1742 Tubacin (Tubulin Acetylation Inducer)
Tubacin (Tubulin Acetylation Inducer)
is a highly potent and reversible cell
-permeable inhibitor of HDAC6 with
IC50 of 0.004μM.
M1748 LBH589 (NVP-LBH589, Panobinostat)
LBH589 (Panobinostat) is a novel broad-spectrum HDAC inhibitor
for MOLT-4 and Reh cells with IC50 of 5 and 20nM, respectively.
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M1670 Belinostat (PXD101, PX105684)
Belinostat is a novel HDAC
inhibitor with IC50 of 27nM.
M1708 EX 527 (SEN0014196)
EX 527 is a potent and selective SIRT1
class III histone deacetylase enzyme
inhibitor with an IC50 of 38 nM.
M1738 Niltubacin (MAZ-1391)
Niltubacin, as an inactive derivative of
Tubacin, is a highly potent and selective
reversible cell-permeable inhibitor of
HDAC6.
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M1753 Trichostatin A (TSA)
Trichostatin A (TSA) is a potent, reversible inhibitor of mammalian
histone deacetylase (HDAC) with IC50 value around 20 nM.
M1775 Tubastatin A hydrochloride
Tubastatin A is a potent and selective HDAC6
inhibitor with IC50 values of 15 nM.
M1778 SB939 (Pracinostat)
SB939 is a novel potent and
orally active histone deacetylase
with high tumor exposure and
efficacy in mouse models of
colorectal cancer.
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PI3K/Akt/mTORDNA Damage
M1791 MS-275 (Entinostat, SNDX-275)
MS-275 is an inhibitor of histone deacetylases (HDACs) that
preferentially inhibits HDAC1 (IC50 = 300 nM) over HDAC3
(IC50 = 8 μM).
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DNA Damage
M2007 Romidepsin (FK228)
Romidepsin (FK228) is a structurally unique,
potent HDAC1 and HDAC2 inhibitor with
IC50 of 36 nM and 47 nM, respectively.
M1790 MGCD0103 (Mocetinostat)
MGCD0103 is a novel HDAC inhibitor, highly specific for classes
I and IV HDACs, with IC50 of 0.15, 0.29 and 1.66μM for HDAC 1,
HDAC 2 and HDAC 3 respectively.
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M1813 PCI-24781 (CRA-024781)
PCI-24781 is a novel and potent histone
deacetylase (HDAC) inhibitor with IC50
value of 0.43 to 2.7 μM.
M2101 PCI-34051
PCI-34051 is a potent HDAC 8
inhibitor with IC50 of 0.01 μM.
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M2111 CUDC-907
CUDC-907 is a potent, orally-available
small molecule dual PI3K and HDAC
inhibitor.
M1876 Valproic acid sodium salt
Valproic acid (VPA) is a histone deacetylase
inhibitor which is reported to enhance central
GABAergic neurotransmission and inhibit Na+
channels.
M2014 MC1568
MC1568 is a selective class
II (IIa) histone deacetylas
(HDAC II) inhibitor with IC50
of 220 nM cells.
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M1993 Droxinostat
Droxinostat is a selective inhibitor of
HDAC3, HDAC6 and HDAC8 with
IC50 of 16.9μM, 2.47μM and 1.46μM,
respectively.
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M1780 Vorinostat (SAHA, Zolinza, MK-0683)
Vorinostat (SAHA, Zolinza, MK-0683) is a selective and potent
histone deacetylase (HDAC) inhibitor with the IC50 value of 10
nM for HDAC-1.
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M2095 Resminostat (4SC-201, RAS2410)
Resminostat is a potent inhibitor of
HDACs 1, 3 and 6 [50% inhibitory
concentration (IC50)=43-72 nmol/l]
representing HDAC classes I and II.
Size:
Size:
M2119 JNJ-26481585 (Quisinostat)
JNJ-26481585 (Quisinostat) is a novel
second-generation class I HDAC inhibitor.
HOT
HOT
NEW
NEW
NEW

DNA Damage
M1785 INO-1001 (3-Aminobenzamide)
INO-1001 is a novel poly(ADP-ribose) polymerase
(PARP) inhibitor with an IC50 of 3 nM.
Size:
M2236 CI-994 (Tacedinaline, PD 123654)
CI-994 (N-acetyl dinaline, PD 123654) is
a novel orally active HDAC inhibitor with
IC50 of 0.57 μM for HDAC1.
M1639 ABT-888 (Veliparib)
ABT-888 (Veliparib) is a potent inhibitor
of PARP-1 and PARP-2 with Ki values
of 5.2nM and 2.9nM respectively.
Size:
M1645 AG14361
AG14361 is a novel poly (ADP-ribose)
polymerase-1 inhibitor with a GI50 of
0.9 μM.
Size:
Size:
DNA Damage
PI3K Inhibitors
M1732 BMN673 (BMN-673, LT-673)
BMN673 is a potent inhibitor of poly
(ADP-ribose) polymerases (PARP)-1
and -2.
M1857 LT-628
LT-628 is the racemate of BMN 673
and LT-674.
Size:
Size:
M2123 Rocilinostat (ACY-1215)
Rocilinostat(ACY-1215) is an HDAC6-selective inhibitor with IC50
of 5 nM.
Size:
M1664 AZD2281 (Olaparib, KU-0059436)
AZD2281(Olaparib, KU-0059436) is a potent PARP (poly ADP
-ribose polymerase) inhibitorwith IC50 of 5 and 1 nM for PARP
-1and PARP-2 respectively.
M1858 LT-674
LT-674 inhibits PARP-1 with an IC50
of 144 nM.
M1972 Iniparib (BSI-201, NSC-746045)
Iniparib is an irreversible, noncompetitive
inhibitor of PARP1 that disrupts binding
between PARP1 and DNA by interacting
with the DNA binding domain.
M2010 BSI-401
BSI-401 is a novel poly (ADP ribose)
polymerase-1 inhibitor.
Size:
PPAI3KR PIn hInibhitoibrsitors
M1644 AG-014699 (PF-01367338, Rucaparib)
AG-014699 (PF-01367338, Rucaparib)
is a PARP inhibitor with a Ki of 1.4 nM.
Size:
Size:
Size:
Size:
M2056 PJ34 hydrochloride
PJ34 is a novel potent inhibitor
of poly(ADP-ribose) polymerase
(PARP) with EC50 of 20 nM.
Size:
HOT
HOT
HOT

PI3K/Akt/mTORDNA Damage
DPIN3KA /InRhNibAito Srsynthesis Inhibitors
M2215 MK-4827 (Niraparib)
MK-4827 is a novel potent, orally
bioavailable PARP-1 and PARP-2
inhibitor with IC50 of 3.8 and 2.1nM,
respectively.
M1801 KU-55933
KU-55933 is a cell-permeable ATP
-competitive inhibitor of ATM (IC50
= 13 nM; Ki = 2.2 nM)with selectivity
over other PIKK family kinases (IC50
= 2.5, 9.3, 16.6 μM for DNAPK, mTOR,
PI 3-K, respectively; IC50 > 100 μM
for PI 4-K and ATR).
Size:
M2290 Oxaliplatin (Eloxatin)
Oxaliplatin inhibits DNA synthesis by
conforming DNA adducts.
DNA Damage
M2216 Dacarbazine (Imidazole Carboxamide)
Dacarbazine is a triazine antineoplastic
agent that is used for DNA methylation
via formation of methyl adducts.
Size:
M1998 KU-60019
KU-60019 is a potent ATM kinase inhibitor with IC50 of 6.3 nM.
M2288 Carboplatin (Paraplatin)
Carboplatin is a DNA synthesis inhibitor
by binding to DNA and interfering with
the cell's repair mechanism.
Size:
M2289 Adrucil (5-FU, Carac, Efudex)
Adrucil(Fluorouracil) belongs to the family
of drugs called antimetabolites.
M2047 VE-821
VE-821 is a highly selective and potent
ATR inhibitor with IC50 of 26 nM.
Size:
M2187 ETP-46464
ETP-46464 is a potent inhibitor against
mTOR, ATR, DNA-PK, PI3-Kα and ATM
with IC50 of 0.6, 14, 36, 170 and 545nM,
respectively.
Size:
M2224 Raltitrexed
Raltitrexed is an inhibitor of
thymidylate synthase used
in cancer chemotherapy.
Size:
M2291 Azacitidine (5-azacytidine, Mylosar)
Azacitidine is a nucleoside analogue of
cytidine that specifically inhibits DNA
methylation by trapping DNA methyl
-transferases.
Size:
APIT3MK /InAhTibRit oIrnshibitors
M2309 CP-466722
CP-466722 is an potent and reversible
ATM inhibitor.
Size:
Size:
M2223 Cisplatin (Cisplatinum)
Cisplatin is a potent anticancer agent
that blocks DNA synthesis.
Size:
Size:
Size:
Size:
NEW
NEW
NEW

DNA Damage
M2057 Dexrazoxane HCL (Cardioxane)
Dexrazoxane hydrochloride is a
Topoisomerase II inhibitor and
intracellular ion chelator.
Size:
M2292 CX-5461
CX-5461 selectively inhibits Pol
I-driven transcription of rRNA
with IC50 of 142 nM in HCT-
116 cells.
M2327 Daunorubicin HCL (Daunomycin HCL)
Daunorubicin HCl inhibits both DNA
and RNA synthesis and inhibits DNA
synthesis with Ki of 0.02 μM.
Size:
M1969 Doxorubicin (Adriamycin, Rubex)
Doxorubicin is an anthracycline antibiotic
that inhibits DNA topoisomerase II used
in cancer chemotherapy.
DNA Damage
PI3K Inhibitors
M2001 Idarubicin
Idarubicin is an anthracycline antibiotic
and a DNA topoisomerase II (topo II)
inhibitor for MCF-7 cells.
M2089 Irinotecan hydrochloride trihydrate
Irinotecan hydrochloride trihydrate is a potent inhibitor of DNA
topoisomerase I.
M2292 Cytarabine
Cytarabine (Cytosine arabinoside, AraC) is
an antimetabolic agent and DNA synthesis
Size:
M1982 Amonafide (AS1413, Quinamed)
Amonafide is a unique ATP-independent
Topo II inhibitor that is being studied in the
treatment of cancer.
M2144 Topotecan HCL (NSC 609669)
Topotecan hydrochloride is a
topoisomerase I inhibitor and
an apoptosis inducer.
M2199 Camptothecin
Camptothecin is a cytotoxic quinoline
alkaloid which inhibits the DNA enzyme
topoisomerase I (topo I).
M2217 Mitoxantrone dihydrochloride
Mitoxantrone dihydrochloride is a
potent inhibitor of topoisomerase II.
DPIN3KA -InPhKib iItnorhsibitors
Size:
Size:
Size:
M2326 Etoposide (Vepesid)
Etoposide is a semisynthetic derivative
of podophyllotoxin, which inhibits DNA
synthesis via topoisomerase II inhibition
activity.
Size:
M2308 NU7026
NU7026 is a DNA-PK inhibitor with IC50
of 0.23 μM.
Size:
TPoI3pKo Inishoibmitoerrsase Inhibitors
Size:
Size:
Size:
Size:
Size:

PI3K/Akt/mTOREpigenetics
M1824 SRT1720
SRT1720 is a selective small molecule
activator of SIRT1 that is 1,000-fold
more potent than resveratrol (EC1.5
= 0.16 versus 46.2 μM,respectively).
Size:
Epigenetics
M2167 (+)-JQ1
(+)-JQ1 is a potent, high affinity, selective
BET bromodomain inhibitor.
M2024 BIX 01294
BIX 01294 is a potent inhitor of G9a
histone methyltransferase with IC50
of 2.7 μM.
M2179 EPZ-5676
EPZ-5676 is a potent and selective
aminonucleoside inhibitor of DOT1L
histone methyltransferase.
M2182 RG108
RG108 is a novel small-molecule inhibitors
of DNA methyltransferases with IC50 of 115
nM.
Size:
M2219 RVX-208
RVX-208 is a first-in-class, small
molecule inhibitor of BET bromo
domain with IC50 of 0.51 μM for
BD2.
Size:
Size:
HPIi3sKto Innheib ditoerms ethylases Inhibitors
M2096 GSK1210151A (I-BET151)
GSK1210151A (I-BET151) is an inhibitor
of the BET family with IC50 of 0.5 μM, 0.25
μM and 0.79 μM for BRD2, BRD3 and
BRD4, respectively.
Size:
M2190 I-BET-762 (GSK525762)
I-BET-762 (GSK525762) is a selective
small molecule BET inhibitor.
M2334 EPZ004777
EPZ004777 is a potent, selective, small
-molecule inhibitor of DOT1L with IC50
of 0.4 nM.
SPiI3rtKu Iinnh iIbnithoirbsitors
M2275 JIB-04
JIB-04 is a selective inhibitor of Jumonji
histone demethylase with IC50 values of
230, 340, 435, 445, 855 and 1100 nM
for JARID1A, JMJD2E, JMJD2B, JMJD2A,
JMJD3 and JMJD2C respectively.
DPIN3KA InMheibtihtoyrlstransferase Inhibitors
M2052 Decitabine (NSC 127716)
Decitabine is a potent inhibitor of DNA
methylation for the treatment of myelody
-splastic syndromes.
EPpI3iKg Iennheibtiitcor Rs eader Domain Inhibitors
Size:
Size:
HPIi3sKto Innheib Mitoertshyltransferase Inhibitors
Size:
Size:
Size:
Size:

NF-κB
NF-κB
Stem Cells & Wnt
HPIe3dKg PI3K Inehhiboigto Inhibitors
rIsnhibitors
IIκκBB//IIKKKKrs Inhibitors
M2040 Bay 11-7082 (Bay 11-7821)
Bay 11-7082 is an inhibitor of cytokine
-induced IκB-α phosphorylation (IC50
~ 10 μM).
Size:
M1713 GDC-0449 (Vismodegib, HhAntag691)
GDC-0449 (Vismodegib) is a potent,
specific hedgehog pathway inhibitor
with IC50 values of 1.4 and 3.0μM
for inhibition of ABCG2 and Pgp
respectively.
HOT
Size: 10mg 50mg 200mg >500mg Inquiry
M1812 GANT58 (Adriamycin, Rubex)
GANT58 is a cell-permeable GLI antagonist
that inhibits GLI1-induced transcription (IC50
= 5 μM).
Size:
M1874 Purmorphamine
Purmorphamine is a small molecule Hh
agonist which activates the hedgehog
pathway by directly binding to SMO.
Size:
M1975 Cyclopamine
Cyclopamine is a naturally occuring steroidal
alkaloid that causes cyclopia by blocking sonic
hedgehog signaling.
Size:
M2110 LY2940680
LY2940680 is a potent Hedgehog inhibitor
with potential anticancer activity.
M2060 SC-514 (GK 01140)
SC-514 is a selective and reversible
inhibitor of IκB kinase 2 (IKK2) with
IC50 of 3-12 μM.
Size:
M2300 TPCA-1 (Niraparib)
TPCA-1 is an inhibitor of IKK-2 with
IC50 of 17.9 nM.
NEW
Size:
M2336 BMS-345541 hydrochloride
BMS-345541 hydrochloride is a selective
inhibitor of the catalytic subunits of IKK
(IC50 values of 0.3 μM and 4 μM for
IKK-2 and IKK-1 respectively).
Size:
NIκFB-/IκKBK rIsnhibitors
M2197 Sulfasalazine (Salazopyrin)
Sulfasalazine is an inhibitor of NF-κB
activation and a prodrug of the anti-inflammatory
agent 5-aminosalicylic
acid.
Size:
NEW
M2298 QNZ (EVP4593)
QNZ is an inhibitor of NF-κB activation
with IC50 of 11 nM.
Size:
Size:
NEW

PI3K/Akt/mTORNeuronal Signaling
M1930 Granisetron hydrochloride
Granisetron hydrochloride is a potent
and selective 5-HT3 receptor antagonist
that possesses potent antiemetic activity.
Size:
Neuronal Signaling
M2231 Dimebon dihydrochloride
Dimebon dihydrochloride is a non-selective
antihistamine that displays
cognitive enhancing abilities.
M2279 Citalopram HCL (Celexa, Cipramil)
Citalopram (Celexa, Cipramil) is an
antidepressant drug.
M1830 Firocoxib
Firocoxib is a selective COX-2 inhibitor
exhibiting high selectivity to inhibit COX-2.
M2146 Prucalopride
Prucalopride is a potent, selective
and specific serotonin 5-HT4 receptor
agonist with enterokinetic properties.
Size:
M2263 Ondansetron HCL (GR 38032, SN 307)
Ondansetron hydrochloride is a
5-HT3 receptor antagonist with
Ki of 6.16 nM.
Size:
Size:
M2175 Palonosetron hydrochloride
Palonosetron hydrochloride is a novel
antiemetic 5-HT3-receptor antagonist.
M2262 Mianserin hydrochloride (Bolvidon)
Mianserin hydrochloride is a non-selectivE
5-HT2 receptor antagonist.
M1965 Celecoxib (Celebrex, Celebra)
Celecoxib is a selective COX-2 inhibitor
(IC50 values are 15 and 0.04μM for COX
1 and COX-2 respectively).
5P-IH3KT I nRheibciteoprstor Inhibitors
M2048 Sumatriptan succinate (GR-43175)
Sumatriptan succinate is a 5-HT1 serotonin receptor agonist.
M2134 Vortioxetine hydrobromide
Vortioxetine hydrobromide (Lu AA21004)
is a 5-HT3, 5-HT7 and 5-HT1D receptor
antagonist, a 5-HT1B receptor partial
agonist, a 5-HT1A receptor agonist and
a 5-HT transporter (5-HTT) inhibitor in vitro.
Size:
CPIO3KX I nInhhibiibtoirtsors
Size:
Size:
M2131 SB-269970 HCL(SB269970A)
SB-269970 hydrochloride is a potent and
selective 5-HT7 receptor antagonist with
pKi of 8.3.
Size:
Size:
M2230 Agomelatine (Valdoxan, Melitor)
Agomelatine is a metabolically stable analog
of melatonin that displays agonist activity for
MT1 and MT2 binding with nanomolar affinity.
Size:
Size:
Size:
Size:
Size:
M2233 Nepafenac
Nepafenac is an analgesic selective
inhibitor of COX-2.

AbMole Inhibitor catalog July 2014

AbMole Inhibitor catalog July 2014

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AbMole Inhibitor catalog July 2014