AbMole Inhibitor catalog July 2014

July 2014

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PI3K

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Free Sample Program

AbMole Bioscience concentrates on providing our customers industry-leading quality

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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

Angiogenesis FLT3 ................................................................... 15

Src-bcr-Abl ......................................................... 15

Syk ..................................................................... 16

HIF...................................................................... 15

BTK .................................................................... 16

FAK .................................................................... 16

JAK/STAT JAK..................................................................... 19

Pim ..................................................................... 20

STAT .................................................................. 20

Protein Tyrosine Kinase VEGFR/PDGFR.................................................. 7

EGFR/HER2....................................................... 10

c-Met .................................................................. 12

IGF-1R................................................................ 14

ALK..................................................................... 13

Apoptosis Bcl-2 .................................................................. 17

p53 .................................................................... 17

TNF-alpha .......................................................... 17

Caspase ............................................................ 18

Mdm2 ................................................................. 18

IAP...................................................................... 18

MAPK MEK.................................................................... 20

p38 MAPK .......................................................... 21

Raf ...................................................................... 22

JNK..................................................................... 22

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Cytoskeletal Signaling HSP90 ................................................................ 23

Kinesin................................................................ 25

Wnt/beta-catenin ................................................ 25

Microtubule......................................................... 24

Integrin ............................................................... 25

TGF-beta/Smad TGF-beta ............................................................ 30

PKC .................................................................... 30

Epigenetics Epigenetic Reader Domain ................................ 36

Histone demethylases ........................................ 36

DNA Methyltransferase ...................................... 36

Histone Methyltransferase .................................

Cell Cycle Aurora Kinase..................................................... 26

CDK.................................................................... 27

Checkpoint ......................................................... 28

PLK..................................................................... 29

ROCK ................................................................. 29

Wee1 .................................................................. 29

DNA Damage HDAC ................................................................ 31

PARP.................................................................. 33

ATM/ATR............................................................ 34

DNA/RNA Synthesis........................................... 34

Topoisomerase................................................... 35

Sirtuin ................................................................. 36

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

Transmembrane Transporters Sodium Channel ................................................. 43

P-gp.................................................................... 43

ATPase............................................................... 43

Potassium Channel ............................................ 43

CFTR...................................................................43

Endocrinology & Hormones GPR.................................................................... 42

Estrogen Receptor ............................................. 42

Androgen Receptor ............................................ 42

Metabolism PPAR.................................................................. 45

CYP17 ................................................................ 44

PDE .................................................................... 45

CETP.................................................................. 44

HMG-CoA........................................................... 45

Transferase ........................................................ 45

Dehydrogenase .................................................. 44

Factor Xa............................................................ 44

Monoamine Oxidase .......................................... 45

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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

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PI3K InhibitorsPI3K Inhibitors

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M1671 BEZ235 (NVP-BEZ235)

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M1651 AS605240

AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) with an IC50 of 8 nM.

M1680 BKM120 (NVP-BKM120)

BKM120 (NVP-BKM120) is a potent and highly specific oral pan-class I PI3K inhibitor.

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M1727 GDC-0980 (RG7422)

GDC-0980(RG7422) is a potent,highly selective, oral, dual inhibitorof class I PI3K and mTOR.

M1715 GDC-0941

GDC-0941 is a potent inhibitor of PI3Kα/δwith IC50 of 3 nM, with modest selectivityagainst p110β (11-fold) and p110γ (25-fold).

M2220 GDC-0941 Bimesylate

GDC-0941 Bimesylate is the orally bioavailable bismesylate salt of a potent inhibitor PI3K.

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M1735 BGT226 (NVP-BGT226)

BGT226(NVP-BGT226) is a novel phosphoinositide 3-kinase/mTOR dual inhibitor.

M1736 CH5132799

CH5132799 is a novel and potentclass I PI3K inhibitor with IC50value of 0.014 μM.

M1739 PKI-179

PKI-179 is an orally dual phosph-atidylinositol-3-kinase (PI3K)/mammalian target of rapamycin(mTOR) inhibitor with potentialantineoplastic activity.

M1770 PIK-75 Hydrochloride

PIK-75 Hydrochloride is a PI3Kp110α specific inhibitor with IC50s of 6,1300,76,510 nMfor p110α,p110β,p110γ, p110δrespectively.

M1772 PKI-587 (PF-05212384)

PKI-587(PF-05212384) is a highlypotent dual PI3K/mTOR kinase inhibitor with the IC50 value of 0.4nM.

M1773 PI-103

PI-103 is a potent, ATP-competitivePI3K,cell-permeable,inhibitor.TheIC50 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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BEZ235 (NVP-BEZ235) is a potent dualPI3K and mTOR inhibitor of p110α, p110γ,p110δ and p110β with IC50 of 4 nM, 5 nM,7 nM and 75 nM, respectively.

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M1849 XL765 (SAR245409)

XL765 is a PI3K/mTOR dual kinase inhibitor with IC50 values of 157 nM,39 nM, 113 nM, 9 nM and 43nM for mTOR, p110α, p110β,p110γ and p110δ, respectively.

M1809 NU7441 (KU 57788)

NU7441 (KU 57788) is a potent andselective DNA-dependent proteinkinase (DNA-PK) inhibitor with IC50values of 14, 1700, 5000,>100000 and >100000 nM for DNA-PK, mTOR,PI 3-K, ATM and ATR respectively.

M1788 IC87114 (PIK-293)

IC87114 is a compound that inhibitsthe p110δ isoform of PI3K selectively,p110δ (IC50 = 0.13 µM) vs. p110α(IC50 = 200 µM), p110β(IC50 = 16 µM)and p110γ(IC50 = 61 µM).

M1795 TGX-221

TGX-221 is a potent and specific cellpermeable inhibitor of PI3K,p110β(IC50 = 10nM).

M1819 A66

A66 is a potent and specific inhibitorof PI3K p110α with IC50 values of 32,30 and 43 nM for p110α, p110α/E545Kand p110α/H1047R.

M1878 ZSTK474

ZSTK474 is an ATP-competitive inhibitorof PI3K, induces G1 arrest of the cell cyclein vivo.

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M1879 XL147 (SAR245408)

XL147 (SAR245408) is an orally selective small molecule Class IPI3K kinase family inhibitor.

M1886 TG100-115

TG100-115 is a selective PI3K γ/δinhibitor with IC50 values of 83 and235 nM respectively.

M1896 PIK-90

PIK-90 is a novel and potent PI3Kinhibitor with IC50 values of 11 nM,350 nM, 18 nM and 58 nM for p110α,p110β, p110γ and p110δ respectively.

M1925 LY294002

LY294002 is a highly selective PI3Kinhibitor with IC50 values of 0.31, 0.73, 1.06 and 6.60μM for PI3Kβ, PI3Kα, PI3Kδ and PI3Kγ respectively.

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M1931 GSK2126458

GSK2126458 is a highly potent inhibitorof PI3K and mTOR with low picomolarto subnanomolar activity.

M1933 GNE-493

GNE-493 is a potent, selective and orally available pan-PI3-kinase anddual pan-PI3-kinase/mTOR inhibitorfor the treatment of cancer.

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PI3K InhibitorsPI3K InhibitorsM1945 CAL-101 (GS-1101)

CAL-101 (GS-1101) is an oral PI3Kδ-specific inhibitor that has shownpreclinical and clinical activity in non-Hodgkin lymphoma and chroniclymphocytic leukemia.

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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 AKTT308 and AKT S473, respectively.

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M2073 IPI-145

IPI-145 is a potent, oral inhibitor of PI3Kdelta and PI3K-gamma.

M2050 GSK2636771

GSK2636771 is a potent, orally availableand specific PI3K p110β(PI3K beta,PI3Kβ)inhibitor.

M2053 Wortmannin (SL-2052)

Wortmannin is a specific, covalentinhibitor of phosphatidylinositol 3-kinase(PI 3-kinase) with IC50 of 3 nM.

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M2104 BYL719

BYL719 is the first oral PI3Kinhibitor that strongly andselectively inhibits the PI3Kalpha isoform of PI3K.

M2135 GDC-0032

GDC-0032 is a potent, nextgeneration PI3-kinase inhibitor.

M2295 AZD6482

AZD6482 is an inhibitor of PI3Kβwith IC50 of 21 nM.

M2296 3-Methyladenine (3-MA)

3-Methyladenine (3-MA) is a selective PI3Kinhibitor for Vps34 and PI3Kγ with IC50 of25 μM and 60 μM, respectively.

M1654 AT7867

AT7867 is a potent and oral inhibitor ofAKT and p70 S6 kinase with an IC50 of17 nM.

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M1978 GSK1059615

GSK1059615 is a potent, ATP-competitiveinhibitor of PI 3-kinase alpha (PI3Kα) withIC50 of 2 nM.

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PI3K InhibitorsAkt Inhibitors

M1789 GSK690693

GSK690693 is a potent Akt inhibitor(Akt1 IC50= 2 nM, Akt2 IC50 = 13 nM,Akt3 IC50 = 9 nM).

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M1862 GDC-0068 (RG7440)

GDC-0068 (RG7440) is a potent and selective, ATP-competitive Akt inhibitor with IC50 valuesof 5 to 18 nM.

M1823 Perifosine (KRX-0401, NKA17)

M1837 MK-2206

MK-2206 is a novel allosteric inhibitor ofAkt with IC50 values of 8 nM, 12nM and65nM for Akt1, Akt2 and Akt3, respectively.

Perifosine is an orally active Akt inhibitor, the antiproliferativeproperties of Perifosine with an IC50 of 0.6–8.9 µM.

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.

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M1703 Deforolimus (Ridaforolimus, AP23573)

Deforolimus (also known as AP23573 and MK-8669) is aninvestigational targeted and small-molecule mTOR inhibitor.

M1709 Everolimus (RAD001, Certican)

Everolimus (RAD001) also known as SDZ-RAD and Certican isan mTOR inhibitor with IC50 of 0.63 nM.

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AZD8055 is a novel ATP-competitive inhibitor of mTOR kinase with an IC50of 0.8 nM.

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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).

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M2303 AZD5363

AZD5363 is a potent Akt inhibitor for Akt1,Akt2 and Akt3 with IC50 of 3 nM, 8 nMand 8 nM, respectively.

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PI3K InhibitorsPI3K InhibitorsM1731 KU-0063794 (GS-1101)

KU-0063794 is a potent and selectivemTOR inhibitor with IC50 values ofapproximately 10 nM for mTORC1and mTORC2.

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M1760 Palomid 529 (P529)

Palomid 529(P529) is a novel potent PI3K/Akt/mTOR inhibitorand shows a potent antiproliferative activity in the NCI-60 celllines panel, with growth inhibitory 50(GI50) <35 μM.

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.

M1852 WAY-600

WAY-600 is a selective single digitnanomolar ATP-competitive mTORinhibitor with an IC50 of about 9 nM.

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M2022 Torin 2

Torin 2 is a potent and selective mTOR inhibitor with IC50 of 2.1nM.

M2094 GDC-0349 (RG7603)

GDC-0349 is a potent and selective, ATP-competitive mTOR inhibitor.

M2099 OSI-027

OSI-027 is an orally bioavailable,potent and selective inhibitor of mTORC1 and mTORC2 withIC50 values of 22 nM and 65nM, respectively.

M2118 XL388

XL388 is a novel, highly potent, ATP-competitive and orally bioavailable mTOR inhibitor.

M2151 INK128 (MLN0128)

INK128(MLN0128) is a potent and selectivedual TORC1/2 inhibitor with IC50 of 1 nM.

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M1981 PP242

PP242 is a selective, ATP-competitivemTORC1/mTORC2 inhibitor with IC50of 8 nM.

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M1756 WYE-687

WYE-687 is a novel ATP-competitive and selective inhibitors of the mammalian targetof rapamycin(mTOR) with an IC50 of 7 nM.

M1755 WYE-354

WYE-354 is a cell-permeable pyrazolopyrimidinecompound that acts as a potent and ATPcompetitive mTOR inhibitor (IC50 = 5 nMwith S6K as the substrate and 100 µM ATP).

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M1692 CHIR-99021 (CT99021)

CHIR-99021 is an aminopyrimidinederivative that inhibits GSK3α andGSK3β with IC50 values of 10 and6.7 nM, respectively.

M2299 AZD2014

AZD2014 is a novel dual mTORC1and mTORC2 inhibitor with potentialantineoplastic activity.

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M1848 OSU-03012

OSU-03012 is a novel and potentinhibitor of PDK-1 with an IC50 of 5 µM.

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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.

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M2304 TWS119

TWS119 is a GSK-3β inhibitorwith IC50 of 30 nM.

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M2178 AZD2858

AZD2858 is a potent, orally bioactive inhibitor of GSK-3.

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PI3K InhibitorsPDK1 Inhibitors

PI3K InhibitorsGSK-3 Inhibitors

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.

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M2184 Indirubin

Indirubin is a potent cyclin-dependent kinasesand GSK-3β inhibitor with IC50 of ~75 nMand 0.19 μM.

M2305 CHIR-98014

CHIR-98014 is a potent andselective GSK-3 inhibitor forGSK-3ɑ and GSK-3β withIC50 of 0.65 nM and 0.58nM,respectively.

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M2306 Tideglusib (NP031112, NP-12)

Tideglusib (NP031112, NP-12) is apotent non ATP-competitive inhibitorof GSK3 with IC50 of 60 nM.

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M2115 GSK2334470

GSK2334470 is a highly specificand potent inhibitor of PDK1 withIC50 of 10 nM.

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M2310 BX795

BX795 is a potent and specific TBK1, IKKε and PDK-1 inhibitorwith IC50 of 6 nM, 41 nM and 111 nM, respectively.

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PI3K InhibitorsPI3K InhibitorsM2311 BX-912

BX912 is a selective potent PDK1 inhibitor with IC50 of 12 nM.

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M2271 PF-4708671 (PF-04708671)

PF-4708671 is a novel cell-permeableinhibitor of S6K1 with Ki/IC50 value of20 nM/160 nM.

M1640 ABT-869 (Linifanib)

ABT-869 (Linifanib) is an ATP-competitive,multi-targeted RTKinhibitor that is completelyeffective against all members of VEGFR and PDGFR.

M1643 AEE788 (NVP-AEE 788)

AEE788 (NVP-AEE788) is a novel multitargetedHER 1/2 and VEGFR 1/2 receptor family tyrosinekinases inhibitor with IC50 of 2, 6, 77, 59 nM forEGFR, ErbB2, KDR, and Flt-1.

M1656 AV-951 (Tivozanib)

AV-951 (Tivozanib) is a potent VEGFR-1, 2 and 3, c-Kit and PDGFRinhibitor with IC50 of 0.21, 0.16, 0.24, 1.63 and 1.72 nM respectively.

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PI3K InhibitorsS6 Kinase Inhibitors

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PI3K InhibitorsAMPK Inhibitors

M2238 Dorsomorphin dihydrochloride

Dorsomorphin dihydrochloride is aotent and selective AMPK inhibitorwith Ki value of 109 nM.

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M2308 NU7026

NU7026 is a DNA-PK inhibitor withIC50 of 0.23 μM.

M1948 BI-D1870

BI-D1870 is a small molecule specificinhibitor of the p90 RSK (ribosomalS6 kinase) with an IC50 of 10-30 nM.

PI3K InhibitorsDNA-PK Inhibitors

PI3K InhibitorsVEGFR/PDGFR Inhibitors

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M1658 Axitinib (AG-013736)

Axitinib (AG013736) inhibitsmultiple targets including VEGFR, PDGFR and cKit.

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M1669 Regorafenib (BAY 73-4506)

Regorafenib (BAY 73-4506) is a novel oralmultikinase inhibitor of c-KIT, VEGFR2,B-Rafwith IC50s of 17, 40 and 69 nM respectively.

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M1673 BIBF1120 (Vargatef)

BIBF 1120 (Vargatef) is a novel tripleangiokinase inhibitor of VEGFR, PDGFRand FGFR.

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M1688 Brivanib (BMS-540215)

Brivanib (BMS-540215) is a VEGFR-2inhibitor with an IC50 value of 25nM.

M1687 Brivanib alaninate (BMS-582664)

Brivanib alaninate (BMS-582664) is anovel,orally available and selectivereceptor tyrosine kinase inhibitor ofVEGF-R2 and FGF-R1 and -2.

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M1840 BGJ398 (NVP-BGJ398)

BGJ398 is a potent and selective FGFR kinase inhibitor with IC50values of 0.9 nM, 1.4 nM, 1 nM and 60 nM for FGFR1, FGFR2,FGFR3 and FGFR4, respectively.

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M1697 Dovitinib (TKI258, CHIR-258)

Dovitinib (TKI258, CHIR-258) is asmall-molecule multitargeted receptortyrosine kinase inhibitor.

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M1826 Sunitinib Malate (SU-11248, Sutent)

Sunitinib is a multitargeted tyrosine kinaseinhibitor of VEGFR, PDGFRβ and KITinhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ andKIT, respectively.

M1723 Crenolanib (CP-868596)

Crenolanib(CP-868596) is an orallybioavailable, selective small moleculeinhibitor of PDGFRα and PDGFRβ withIC50 of 0.9 and 1.8 nM respectively.

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M1696 Cediranib (AZD2171)

Cediranib (AZD2171) inhibited VEGFR2 andKDR phosphorylation with IC50s of 0.4 and0.5 nM, respectively.

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M1805 OSI-930

OSI-930 is a multi-targeted tyrosine kinaseinhibitor of the receptor tyrosine kinasesc-Kit and VEGFR-2 with IC50 values of9.5 and 10.1 nM.

M1841 Lenvatinib (E7080)

Lenvatinib (E7080) is a potentinhibitor of multiple tyrosine kinases,including VEGFR3 tyrosine kinase(IC50=5.2 nM) and VEGFR2 tyrosinekinase (IC50=4.0 nM).

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M1842 Pazopanib (GW786034)

Pazopanib is an oral angiogenesisinhibitor of tyrosine kinases, targetingvascular endothelial growth factorreceptor, platelet-derived growthfactor receptor, and c-Kit.

M1827 Sorafenib Tosylate (BAY43-9006)

Sorafenib (BAY 43-9006) is an orally active multikinase inhibitor oftyrosine protein kinases VEGFR/PDGFR and RAF/MEK/ERK withIC50 values of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant BRAF.

M1838 Masitinib (AB1010)

Masitinib is a tyrosine kinase inhibitor targeting stem cell factorreceptor (c-kit) and platelet-derived growth factor (PDGF) receptor.

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PI3K InhibitorsPI3K InhibitorsM1882 Vatalanib dihydrochloride (PTK787)

Vatalanib is a selective small molecule proteinkinase inhibitor of VEGF receptors 1-3.

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M1994 Telatinib (BAY 57-9352)

Telatinib (BAY 57-9352) is an orallyactive small-molecule tyrosine kinaseinhibitor of VEGFR2, VEGFR3 andPDGFRβ with IC50 of 6 nM, 4 nMand 15 nM, respectively.

M1995 Ki8751

Ki8751 is a potent, selective inhibitor of VEGFR-2 tyrosine kinase (IC50=0.9 nM).

M1956 Apatinib (YN968D1)

Apatinib is a small-molecule multitargetedtyrosine kinase inhibitor of VEGFR2 withan IC50 of 2.43 nM.

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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.

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M1936 E-3810

E-3810 is a novel small moleculeinhibitor with potent and selectiveinhibitory activity of the VascularEndothelial Growth Factor (VEGF)receptors 1-3 and of the FibroblastGrowth Factor (FGF) receptors 1-2.

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M1944 CP-547632

CP-547632 is a novel VEGFR-2tyrosine kinase inhibitor with IC50of 11 nM.

M1918 Amuvatinib (MP470)

Amuvatinib (MP470) is a novel receptortyrosine kinase inhibitor that targetsc-KIT and PDGFRα.

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M2011 PP121

PP121 is a dual inhibitor of tyrosineand phosphoinositide kinases.

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M2031 SU5416 (Semaxanib)

SU5416 is a novel small molecule multi-targeted kinase inhibitor of VEGF receptors,c-kit and FLT3.

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M1941 CP 673451

CP 673451 is a potent inhibitor ofplatelet-derived growth factor beta-receptor (PDGFR-beta) with anIC50 of 1 nM.

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M1999 DMXAA (Vadimezan, ASA404)

DMXAA (Vadimezan, ASA404) is a tumor-vascular disrupting agent (tumor-VDA)and competitive inhibitor of DT-diaphorasewith Ki of 20 μM and IC50 of 62.5 μM, respectively.

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M2074 NVP-BHG712 (BHG712)

NVP-BHG712 is a very potent, selectiveinhbitor of the receptor tyrosine kinaseEphB4 (ED50 = 25 nM).

M1749 Gefitinib (ZD-1839, Iressa)

Gefitinib (ZD-1839, Iressa) is a novelpotent EGFR tyrosine kinase inhibitorwith an IC50 of 0.40nM.

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M1699 CP-724714

CP-724714 is a potent and selective orallyactive HER-2 tyrosine kinase inhibitor, IC50 = 3 nM.

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M1684 BMS-599626 (AC480)

BMS-599626 (AC480) is an orally bioavailable pan-HER tyrosinekinase inhibitor with potential antineoplastic activity.

M1784 Icotinib (BPI-2009H)

Icotinib (BPI-2009H) is a potent andnovel epidermal growth factor receptor(EGFR) tyrosine kinase inhibitor (TKI)with an IC50 of 5 nM.

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M1802 Lapatinib Ditosylate (Tykerb)

Lapatinib Ditosylate is a selective and effective inhibitor of EGFRkinase (Ki = 3 nM),ErbB-2 kinase (Ki = 13 nM) and ErbB-4 kinase(Ki = 347 nM).

M1705 Erlotinib HCL (Tarceva, CP-358774)

Erlotinib is an inhibitor of human EGFR tyrosine kinase (IC50 = 2 nM) and decreases EGFR autophosphorylationin tumor cells (IC50 = 20 nM).

M1721 AZD4547

AZD4547 is a potent, selective and orally active pan-FGFRinhibitor with IC50s of 0.2. 2.5, 1.8 and 165 nM for FGFR1, 2,3 and 4, respectively.

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M2078 SAR131675

SAR131675 is a potent and selectiveVEGFR-3 inhibitor with IC50 of 20 nM.

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M2194 SU5402

SU5402 is a potent and selective VEGFRand FGFR inhibitor with IC50 values of0.02, 0.03, 0.51 and > 100 μM forVEGFR2, FGFR1, PDGFRβ and EGFRrespectively.

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M2153 TSU-68 (SU6668)

TSU-68 (SU6668) is a protein kinase inhibitorof PDGF-Rβ, VEGF-R2 and FGF-R1 with IC50of 0.06, 2.4 and 3.0 μM, respectively.

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PI3K InhibitorsEGFR/HER2 Inhibitors

M1667 AZD8931

AZD8931 is an equipotent, reversible inhibitorof Signaling by EGFR, ERBB2 (HER2), andERBB3 with IC50 of 4, 3, 4 nM respectively.

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PI3K InhibitorsPI3K InhibitorsM1850 WZ4002

WZ4002 is a novel, selective EGFR kinaseinhibitor against EGFR T790M (mutation ofthe gatekeeper T790 residue) with IC50 of8 nM.

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M1943 Canertinib (CI-1033, PD-183805)

Canertinib (CI-1033) is an irreversibletyrosine-kinase inhibitor with activityagainst EGFR (IC50 0.8 nM), HER-2(IC50 19 nM) and ErbB-4 (IC50 7nM).

M1919 Mubritinib (TAK-165)

Mubritinib (TAK-165) is a new potent inhibitor ofhuman epidermal growth factor receptor 2 (HER2)tyrosine kinase(IC50 = 6 nM).

M1869 Dacomitinib (PF-00299804)

Dacomitinib (PF-00299804) is an oral, irreversible,small molecule inhibitor of human epidermal growthfactor receptor-1, -2, and -4 tyrosine kinases.

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M1875 PD173074

PD173074 is a selective FGFR1 andFGFR3 inhibitor with IC50 values of 5,21.5, ~100, 17600 and 19800 nM forFGFR3, FGFR1, VEGFR2, PDGFRand c-Src respectively.

M1913 Neratinib (HKI-272)

Neratinib (HKI-272) is an orallyavailable, irreversible inhibitorof Her 2 tyrosine kinase.

M1851 WZ8040

WZ8040 is a novel EGFR inhibitor which suppresses the growth of EGFR-T790M-containing cell lines and inhibits EGFR phosphorylation.

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M2117 CNX-2006

CNX-2006 is a novel irreversibleEGFR inhibitor with IC50 valueof <20 nM.

M2212 CO-1686 (AVL-301, CNX-419)

CO-1686 is a potent, novel inhibitor of EGFR L858R/T790M kinase with Ki of21.5 nM and 303.3 nM, respectively.

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M1904 Pelitinib (EKB-569)

Pelitinib (EKB-569) is an irreversibleEGFR tyrosine kinase inhibitor withIC50 of 38.5 nM.

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M2021 AG 18 (RG-50810, Tyrphostin 23)

AG-18 is an inhibitor of EGF receptorkinase with an IC50 value of 35 μM.

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M2255 Genistein (NPI 031L)

Genistein is a highly specific inhibitorof protein tyrosine kinase (PTK).

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M2312 AG-1478 (Tyrphostin AG-1478)

AG-1478 (Tyrphostin AG-1478) is a selectiveEGFR inhibitor with IC50 of 3 nM.

M1793 JNJ-38877605

JNJ-38877605 is a small-molecule, ATPcompetitive inhibitor of the catalytic activityof c-Met with an IC50 of 4 nM.


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M1765 PF-2341066 (Crizotinib)

PF-2341066 (Crizotinib) is a potent, orallybioavailable, ATP-competitive small-moleculeinhibitor of c-Met kinase and ALK (anaplasticlymphoma kinase) with IC50 values to be 4and 25 nM for C-Met and ALK resepectively.

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M1758 Foretinib (XL880, GSK1363089)

Foretinib (XL880, GSK1363089) is amulti-targeted inhibitor of c-Met andvascular endothelial growth factorreceptor 2 (VEGFR2) with IC50 value of 0.4 nM for c-MET.

M1811 ARQ-197 (Tivantinib)

ARQ-197 (Tivantinib) is a selectiveand oral small-molecule inhibitor ofc-Met with a minimal IC50 value of0.1 μM.

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M1890 SU11274 (PKI-SU11274)

SU11274 is a selective c-Met inhibitor (IC50 = 0.01 μM in vitro).

M1766 PF-04217903 (PF-4217903)

PF-04217903(PF-4217903) is a novel ATP-competitive small moleculeinhibitor of c-Met kinases with the IC50 values from 3.1 nM to142 nM.

M1777 SGX523

SGX523 is an exquisitely selective, ATPcompetitive inhibitor of the MET receptortyrosine kinase with antitumor activity invivo.

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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 nMfor VEGFR2 and Met respectively.

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M1647 AMG-208

AMG-208 is a potent small molecular inhibitorc-Met with an IC50 of 9.3 nM.

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M1745 AMG-458

AMG-458 (AMG458) is a potent,selective inhibitor of c-Met and areceptor tyrosine kinase that isoften deregulated in cancer.

M1682 BMS-777607

BMS-777607 is a selective and potentsmall-molecule met kinase inhibitor withan IC50 of < 0.1μmol/L.

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PI3K Inhibitorsc-Met Inhibitors

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PI3K InhibitorsPI3K InhibitorsM1899 PHA-665752

PHA-665752 is a selective small molecule c-MET inhibitor (Ki of 4nM, IC50 of 9 nM).

M1794 SB431542

SB-431542 is a potent and selectiveinhibitor of the transforming growthfactor-β (TGF-β) type I receptor activinreceptor-like kinase ALK5 (IC50=94nM).

M1743 X-376

X-376 is a potent and highly specific ALK small molecule tyrosinekinase inhibitor.

M1720 AP26113

AP26113 is a highly potentALK inhibitor with IC50 of0.62 nM.

M1901 Golvatinib (E7050)

Golvatinib (E7050) is an orally bioavailabledual kinase inhibitor of c-Met and VEGFR-2tyrosine kinases with potentialantineoplastic activity.

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M1932 GSK1838705A

GSK1838705A is a small-molecule kinaseinhibitor that inhibits IGF-IR and the insulinreceptor with IC50s of 2.0 and 1.6 nmol/L,respectively.

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M1942 CH5424802 (AF802)

CH5424802 is a highly selective, orally active and potent ALKinhibitor with IC50 of 1.9 nM.

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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).

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M2080 INCB28060

INCB28060 is a novel inhibitor of c-MET kinase with IC50 of0.13 nM.

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PI3K InhibitorsALK Inhibitors

M1873 LDN-193189

LDN-193189 is a highly potent small molecule inhibitor ofbone morphogenetic protein (BMP) type I receptors ALK2and ALK3.

M1859 ALK5 Inhibitor II (SJN 2511)

ALK5 Inhibitor is a potent and ATP-competitiveinhibitor of the TGF-β type I receptor ALK5.

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M1946 CEP-28122

CEP-28122 is a highly potent and selective orally active ALK inhibitor.

M1957 BMS-536924

BMS-536924 is an ATP-competitiveIGF-IR and IR inhibitor with IC50 of100 nM and 73 nM respectively.


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M1792 XL228

XL228 is a potent multikinase small-moleculeinhibitor of insulin-like growth factor type 1 receptor (IGF1R).

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M1717 GSK1904529A

GSK1904529A selectively inhibits IGF-IR and IR with IC50s of 27and 25 nmol/L, respectively.

M2025 PQ401

PQ401 is an insulin growth factor-1receptor (IGF-1R) inhibitor.

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M2192 BMS-754807

BMS-754807 is an ATP-competitive dualkinase inhibitor of IGF-1R and IR with IC50sof 1.8 nM and 1.7 nM, respectively..

M1821 OSI-906 (Linsitinib)

OSI-906 (Linsitinib) is a potent, selectivedual ATP-competitive tyrosine kinaseinhibitor of insulin-like growth factor-1receptor (IGF-1R) and insulin receptor(IR) with IC50 values of 35 nM and 75nM respectively.

M1777 SGX523

SGX523 is an exquisitely selective, ATPcompetitive inhibitor of the MET receptortyrosine kinase with antitumor activity invivo.

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M1950 ASP3026

ASP3026 is a novel and selectiveinhibitor for the ALK kinase.

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M2109 AZD3463

AZD3463 is a novel ALK/IGF1R inhibitorwith IC50 value of 22 nM.

M2075 LDK378

LDK378 is a highly selective, orallybioavailable ALK inhibitor with IC50of 0.15 nM.

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PI3K InhibitorsIGF-1R Inhibitors

Angiogenesis


Angiogenesis

PI3K Inhibitors

M1648 AP24534 (Ponatinib)

Ponatinib (AP24534) is a novelpotent, available small moleculemultitargeted kinase inhibitor ofBCR-ABL, PDGFRα,c-Src, c-Kit,FGFR and VEGFR.

M1992 2-Methoxyestradiol (2ME2)

2-Methoxyestradiol is a naturalmetabolite of estradiol acts viaan estrogen receptor-independentmechanism.

M1641 AC220 (Quizartinib)

AC220 (Quizartinib) is a uniquely potentand selective FLT3 inhibitor.

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M1712 FTY720 (Fingolimod)

FTY720 (Fingolimod) is a sphingosine-1-phosphate receptor1 receptor.

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M1799 Imatinib Mesylate (Gleevec, Glivec)

Imatinib Mesylate is a Bcr-Abl tyrosine kinase inhibitor, withIC50 values of 2.9 and 3.9 μM for the inhibition of T-cellproliferation stimulated by PHA and DCs respectively.

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M1815 KW-2449

KW-2449 is a novel multitargetedkinase inhibitor of FLT3, ABL andAurora kinase with IC50 values of6.6 nM, 14 nM and 48 nM.

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M1828 Tandutinib (MLN518, CT53518)

Tandutinib (MLN518), previously knownas CT53518, is an orally active multitargetedtyrosine kinase inhibitor of FLT3, PDGFR and c-Kit.

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PI3K InhibitorsHIF Inhibitors

M1685 Bosutinib (SKI-606)

Bosutinib (SKI-606) is a novelBcr-Abl inhibitor with IC50 valuesof 0.1 to 0.3 umol/L.

M1659 Saracatinib (AZD0530)

Saracatinib (AZD0530) is an orally activesmall molecule Src inhibitor.

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PI3K InhibitorsFLT3 Inhibitors

M1726 FG-4592 (ASP1517)

FG-4592 (ASP1517) is a novelHypoxia Inducible Factor ProlylHydroxylase inhibitor.

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PI3K InhibitorsSrc-bcr-Abl Inhibitors

M1701 Dasatinib (BMS-354825)

Dasatinib is a small molecule inhibitor of both the SRC andBCR/ABL tyrosine kinases.

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Angiogenesis

1

M1825 PCI-32765 (Ibrutinib)

PCI-32765 (Ibrutinib) is a potent, selectiveand orally bioavailable irreversible inhibitorof BTK with IC50 value of 0.46 nM.


Ang

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M1847 Fostamatinib disodium(R788, R935788)

Fostamatinib disodium (R788, R-935788) is apotent, ATP-competitive and selective Sykinhibitor with IC50 of 41 nM.

M2331 PP2 (AG 1879)

PP2 is a selective inhibitor of Src-family tyrosinekinases with >10,000-fold selectivity over ZAP70and JAK2.

M1990 R788 (Fostamatinib)

R788 (Fostamatinib) is a spleen tyrosinekinase (Syk) inhibitor with IC50 of 41 nM.

M2063 P505-15 hydrochloride (PRT062607)

P505-15 (PRT062607) is a novel, highlyselective inhibitor of Syk with IC50 valueof 1-2 nM.

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M1912 Nilotinib (AMN107)

Nilotinib (AMN107) is a small moleculeBcr-Abl kinase inhibitor with IC50 lessthan 30 nM.

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M2313 KX2-391

KX2-391 (KX01) is a highly selective nonATP-competitive Src inhibitor with GI50 of9-60 nM in cancer cell lines .

M1991 Bafetinib (INNO-406, NS-187)

Bafetinib (NS-187, INNO-406) is a novel second-generation dualBcr-Abl/Lyn tyrosine kinase inhibitor.

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PI3K InhibitorsSyk Inhibitors

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M1767 R-406

R406 is an orally bioavailable and selective inhibitor of spleentyrosine kinase (Syk) with the IC50 of 41nM and Ki value of 30nM.

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M2301 NVP-TAE226 (TAE226)

NVP-TAE226, a potent dual FAK/IGF-1R, inhibiting FAK and IGF-1Rwith IC50 of 5.5 nM and 0.14 μM,respectively.

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PI3K InhibitorsFAK Inhibitors

M2302 PF-562271

PF-562271 is a potent, ATP-competitive, reversible inhibitor ofFAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively.

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M2113 AVL-292 (CC-292)

AVL-292 is an oral, potent and selectivesmall molecule covalent inhibitor of Btk(IC50 < 0.5 nM).

HOT

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NEW

NEW

Apoptosis


Apoptosis

PI3K Inhibitors

M2027 Tenovin-1

Tenovin-1 is a small moleculeactivator of p53 transcriptionalactivity.

M2314 TW-37

TW-37 is a novel nonpeptideinhibitor to recombinant Bcl-2,Bcl-xL and Mcl-1 with Ki of0.29μM, 1.11μM and 0.26μM, respectively.

M1637 ABT-263 (Navitoclax)

ABT-263 (Navitoclax) is a potent, orally bioavailable inhibitor ofthe antiapoptotic Bcl-2 family members Bcl-2,Bcl-x (L),and Bcl-w.

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M1962 Lenalidomide (Revlimid, CC-5013)

Lenalidomide is a thalidomide analogknown to display TNF-α secretioninhibition and possesses immuno-modulatory properties.

M2225 Thalidomide (Thalomid)

Thalidomide is a selective inhibitorof tumor necrosis factor α (TNF-α)synthesis.

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M1638 ABT-737

ABT-737 is a potent and selectiveinhibitor of B-cell lymphoma-2family proteins, in small cell lungcancer.

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M1860 AT-101

AT-101(R-(-)-gossypol acetic acid)is a pan small molecule inhibitorof Bcl-2, Bcl-xL, and Mcl-1.

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M2068 JNJ-26854165 (Serdemetan)

JNJ-26854165(Serdemetan) is a novelactivator of p53 capable of inducingapoptosis in cancer cell lines.

M2036 Pifithrin-α

Pifithrin-α is an inactivator of p53 thatblocks p53-dependent transcriptionalactivation and apoptosis.

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PI3K InhibitorsBcl-2 Inhibitors

M2017 ABT-199 (GDC-0199)

ABT-199 is a highly potent, orally BCL-2 inhibitor.

PI3K Inhibitorsp53 Inhibitors

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PI3K InhibitorsTNF-alpha Inhibitors

M1976 Pomalidomide (Actimid, CC-4047)

Pomalidomide is a second generationimmunomodulator,TNF-α inhibitor withIC50 of 13 nM.spectively.

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/Akt/m

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Apoptosis

1

M2315 Necrostatin-1

Necrostatin-1 is a specific RIP1 inhibitorand inhibits TNF-α-induced necroptosiswith EC50 of 490 nM.


Apo

ptos

is

M1847 Fostamatinib disodium(R788, R935788)

Fostamatinib disodium (R788, R-935788) is apotent, ATP-competitive and selective Sykinhibitor with IC50 of 41 nM.

M2331 PP2 (AG 1879)

PP2 is a selective inhibitor of Src-family tyrosinekinases with >10,000-fold selectivity over ZAP70and JAK2.

M1990 R788 (Fostamatinib)

R788 (Fostamatinib) is a spleen tyrosinekinase (Syk) inhibitor with IC50 of 41 nM.

M2063 P505-15 hydrochloride (PRT062607)

P505-15 (PRT062607) is a novel, highlyselective inhibitor of Syk with IC50 valueof 1-2 nM.

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M2313 KX2-391

KX2-391 (KX01) is a highly selective nonATP-competitive Src inhibitor with GI50 of9-60 nM in cancer cell lines .

M1867 PAC-1

PAC-1 is a procaspase-activatingcompound;activates procaspase-3to produce caspase-3 (EC50 = 0.22 μM).

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PI3K InhibitorsSyk Inhibitors

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M1767 R-406

R406 is an orally bioavailable and selective inhibitor of spleentyrosine kinase (Syk) with the IC50 of 41nM and Ki value of 30nM.

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M2301 NVP-TAE226 (TAE226)

NVP-TAE226, a potent dual FAK/IGF-1R, inhibiting FAK and IGF-1Rwith IC50 of 5.5 nM and 0.14 μM,respectively.

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PI3K InhibitorsFAK Inhibitors

M2302 PF-562271

PF-562271 is a potent, ATP-competitive, reversible inhibitor ofFAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively.

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M2113 AVL-292 (CC-292)

AVL-292 is an oral, potent and selectivesmall molecule covalent inhibitor of Btk(IC50 < 0.5 nM).

HOT

NEW

NEW

PI3K InhibitorsCaspase Inhibitors

Mdm2itorsMdm2 Inhibitors

JAK/STAT


JAK

/STAT

PI3K Inhibitors M1787 INCB18424 (Ruxolitinib)

INCB18424 is a potent inhibitor of bothJAK1 and JAK2 with selectivity versusJAK3 and TYK2 (IC50 values of 2.7,4.5, 332, and 19 nM, respectively, inbiochemical assays).

M1733 TG101348

TG101348 is a selective small-moleculeJanus kinase 2(JAK2) inhibitor with IC50of 3 nM.

M1646 AG490 (Tyrphostin AG490)

AG490 (Tyrphostin AG490) is aselective inhibitor of EGF receptortyrosine kinase (IC50 values are 2and 13.5 μM for EGFR and ErbB2respectively).

M1887 TG101209

TG101209 is a novel small molecule, ATP-competitive JAK2-selective kinase inhibitor (IC50 = 6 nM).

M2044 AZD1480

AZD1480 is a novel small-moleculeinhibitor of JAK1/2 with IC50 of 1.3nM and 0.26 nM, respectively.

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M2125 WP1066

WP1066 is a potent, novel inhibitor ofJAK2 and STAT3 with IC50 of 2.3 μMand 2.43 μM in HEL cells.

M1820 Tofacitinib (CP-690550, Tasocitinib)

Tofacitinib (Tasocitinib, CP-690550) isa novel Janus Kinase 3 (JAK-3) kinaseinhibitor with an IC50 value estimatedat 0.2 μM.

M1804 NVP-BSK805 HCL(BSK805)

NVP-BSK805 dihydrochloride isa potent and selective quinoxalineJAK2 inhibitor with IC50 valuesof 0.48, 0.56 and 0.58 nM for JAK2JH1, FL JAK V617F and FL JAK2wt respectively.

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PI3K InhibitorsJAK Inhibitors

M1660 AZ 960

AZ 960 is a novel and specificinhibitor of the JAK2 kinase witha Ki of 0.45nM in vitro.

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M1700 CYT387 (CYT 11387)

CYT387 is a small-molecule, ATP-competitive JAK1/JAK2 inhibitorwith IC50 of 11 and 18 nMrespectively.

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M2039 Baricitinib (INCB28050, LY3009104)

Baricitinib (INCB28050) is an oral JAK1and JAK2 inhibitor with IC50 of 5.9 nMand 5.7 nM, respectively.

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M1754 WP1130

WP1130 is a small moleculardeubiquitinase (DUB) inhibitorand suppresses JAK-Statsignaling pathway.

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1

M2064 CEP-33779

CEP-33779 is a novel, orally active,selective JAK2 inhibitor with IC50 of1.8 nM.


JAK

/STA

T

M2028 Fludarabine

Fludarabine is a STAT1 activationinhibitor and a DNA synthesis inhibitor.

M1661 AZD6244 (Selumetinib, ARRY-142886)

AZD6244(ARRY-142886, Selumetinib)is a potent MEK 1/2 inhibitor with GI50values ranging from 14 to 50 nM.

M1662 AZD8330 (ARRY-424704, ARRY-704)

AZD8330 (ARRY-424704) is a novel,highly efficacious, uncompetitive MEKinhibitor with an IC50 of 7 nM.

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M1782 NSC 74859 (S3I-201)

NSC74859 (S3I-201) is a STAT3 inhibitorand is effective in hepatocellular cancerswith disrupted TGF-beta signaling.

M1779 SGI-1776

SGI-1776 is novel small moleculeinhibitor of PIM kinase activity withIC50 of 7 ± 1.8, 363 ± 27.6 and69 ± 9.2 nM for Pim-1, Pim-2,and Pim-3, respectively.

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M2055 Niclosamide (Niclocide)

Niclosamide is an inhibitor of STAT3with an IC50 value of 0.25 μM.

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M1690 CI-1040 (PD184352)

CI-1040 (PD184352) is a targetedsignal transduction inhibitor of MEKwith a ki value of 300nM in vitro.

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M1744 ARRY-162 (MEK-162, ARRY-438162)

ARRY-162 is a selective,potentinhibitor of MEK and cellular pERK with IC50 of 12 nM and 11nM,respectively.

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M1750 TAK-733

TAK-733 is a potent and selectiveMEK allosteric site inhibitor withIC50 of 3.2nM for the treatmentof cancer.

Mdm2itorsSTAT Inhibitors

PI3K InhibitorsPim Inhibitors

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M2239 SB1317 (TG02)

SB1317 (TG02) is a novel small moleculepotent CDK/JAK2/FLT3 inhibitor.

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PI3K InhibitorsMEK Inhibitors

M1652 AS703026 (MSC1936369B,Pimasertib)

AS703026 is a novel selective MEK1/2inhibitor, and induces pleiotropic anti-myeloma activity in vitro and in vivo.

MAPK

HOT

HOT

MAPK


MA

PK

PI3K Inhibitors M2316 BIX02189

BIX02189 is a selective inhibitorof MEK5 with IC50 of 1.5 nM.

M1977 U0126

U0126 is a potent and highly selectivenon-competitive inhibitor of MAPK/ERKkinase with IC50 of 72 nM for MEK1and 58 nM for MEK2.

M1759 GSK1120212 (JTP-74057, GSK212)

GSK1120212 (JTP-74057) is a highlypotent and selective MEK inhibitor withIC50 values to be 0.7 and 0.9 nM forMEK1 and MEK2 respectively and withlong circulating half-life.

M1781 SB203580 (RWJ 64809, PB 203580)

SB203580 inhibits the IL-2-inducedproliferation of primary human T cells,murine CT6 T cells, or BAF F7 B cellswith an IC50 of 3-5 μM.

M1822 PD98059

PD98059 is a potent and selective inhibitorof mitogen-activated protein kinase kinase(MKK / MEK) with IC50 value of 2-7 μM.

M1675 BIRB796 (Doramapimod)

BIRB 796 (Doramapimod) is a proteinkinase inhibitor of p38 MAPK with Kdof 100pM.

M1763 PD-0325901 (PD325901)

PD-0325901 is a highly potentand selective MEK inhibitor withan IC50 in C26 cells of 0.33nM.

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M1905 PD318088

PD318088 is a non-ATP competitiveallosteric MEK1/2 inhibitor.

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M2136 PH-797804

PH-797804 is a highly selectiveand potent inhibitor of p38 MAPkinase with IC50 of 26 nM.

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M2084 SCH772984

SCH772984 is a novel and selective inhibitor of ERK1/2 withIC50 of 4 nM and 1 nM, respectively.

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M2177 BIX02188

BIX02188 is a novel specific inhibitorof MEK5 which inhibits catalytic functionof purified, MEK5 enzyme.

PI3K Inhibitorsp38 MAPK Inhibitors

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M2062 SB 202190

SB 202190 is a highly selective, and cell permeable inhibitor of p38MAP kinase with IC50 values of 50and 100nM inhibiting p38α and p38β,respectively.

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M2317 VX-702

VX-702 is a highly selective inhibitorof p38 MAPKα with IC50 of 4-20 nM.

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PI3K

/Akt/m

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MAPK

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M2318 LY2228820

LY2228820 is a novel and potentinhibitor of p38 MAPK with IC50of 7 nM.


MA

PK

M1863 RAF265 (CHIR-265)

RAF265 is a novel, orally bioavailable dual inhibitor of RAF kinaseand 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) isa highly selective B-Raf enzyme inhibitor with an IC50 of 44 nMagainst V600E-mutant BRAF.

M1714 GDC-0879

GDC-0879 is a potent and selectiveB-Raf kinase inhibitor with an EC50of 0.75 µM.

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M1783 SB590885

SB590885 is another selective smallmolecule inhibitor of the B-Raf kinaseand Ki app values are 0.16 and 1.72nMfor B-Raf and c-Raf respectively.

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M2045 CEP-32496

CEP-32496 is a potent orallyactive BRAF inhibitor with IC50of 14 nM.

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M2090 MLN2480 (BIIB-024)

MLN2480 (BIIB-024) is an oral,selective pan-Raf kinase inhibitor.

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M2235 TAK-632

TAK-632 is a potent and selective pan-RAF inhibitor.

PI3K InhibitorsRaf Inhibitors

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M1818 ZM 336372

ZM 336372 is a potent, selective ATP-competitive inhibitorof 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 potentialantineoplastic activity.

M1774 PLX4720

PLX4720 is a selective BRAFV600E inhibitorwith the IC50 values of 160nM and 130 nMfor B-Raf and BRK respectively.

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PI3K Inhibitors

M1679 BIIB021 (CNF2024)

BIIB021 (CNF2024) is an orally availablesynthetic non-ansamycin Hsp90 inhibitorwith ki value of 1.7nM.

M2319 AZ628

AZ628 is a potent inhibitor for wild-type CRAF and BRAF V600E withIC50 of 29nM and 34nM,respectively.

M1741 Ganetespib (STA-9090)

Ganetespib (STA-9090) is a potentsynthetic small molecule inhibitor ofHsp90 with potential antineoplasticactivity.

M2013 JNK-IN-8

JNK-IN-8 is a selective JNK inhibitor that inhibits phosphorylationof c-Jun.

M1725 CUDC-305

CUDC-305 is a heat shock protein 90inhibitor of the novel imidazopyridineclass.

M2076 SP600125

SP600125 is a novel and selective inhibitorof c-Jun N-terminal kinase (JNK), inhibitedphosphorylation of c-Jun with an IC50 of 5-10 microM.

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M1798 NVP-HSP990 (HSP990)

NVP-HSP990 is an orally bioavailableinhibitor of human heat-shock protein90 with potential antineoplastic activity.

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PI3K InhibitorsHSP90 Inhibitors

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M1762 AUY922 (NVP-AUY922)

AUY922 (NVP-AUY922) is a smallmolecule Heat Shock Protein 90(HSP90) inhibitor with IC50 valuesof 13 and 21 nM for HSP90α andHSP90β respectively.

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M1908 NVP-BEP800 (VER-82576)

NVP-BEP800 is a novel, fully synthetic,orally bioavailable inhibitor of Hsp90βwith an IC50 of 58 nM.

PI3K InhibitorsJNK Inhibitors

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M1949 AT13387

AT13387 is a novel, high-affinityheat-shock protein 90 (HSP90)inhibitor with IC50 of 18 nM in A375 cells.


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M1892 Vincristine sulfate (leurocristine)

Vincristine(leurocristine) is a mitoticinhibitor used in cancer chemotherapy.

M1940 Docetaxel (Taxotere)

Docetaxel (Taxotere), a semi-syntheticanalog of paclitaxel, is a promoter of microtubule polymerization leading tocell cycle arrest at G2/M, apoptosisand cytotoxicity.Size:


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M2070 XL888

XL888 is a novel small-molecule inhibitor of HSP90 with IC50 of 24nM.

M2003 PF-04929113 (SNX-5422)

PF-04929113 (SNX-5422) isa potent and selective Hsp90inhibitor with Kd of 41 nM.

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M2320 17-AAG (Tanespimycin)

17-AAG (Tanespimycin) is a potentHSP90 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 withKd of 0.4 μM.

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M1970 Paclitaxel (Taxol)

Paclitaxel is a mitotic inhibitor withIC50 of 0.1 pM in human endothelialcells.

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M2321 17-DMAG HCL (Alvespimycin)

17-DMAG (Alvespimycin) is a potentHSP90 inhibitor with IC50 of 62 nM.

M2083 Elesclomol (STA-4783)

Elesclomol (STA-4783) is a small-molecule investigational agent that selectively induces apoptosis in cancer cells by increasingoxidative stress.

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PI3K InhibitorsMicrotubule Inhibitors

M1642 ABT-751

ABT-751 is an orally bioavailable tubulininhibitor with IC50 of about 1.5 and 3.4µM in neuroblastoma and non-neuroblastomacell lines, respectively.

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PI3K Inhibitors

M1796 XAV939

XAV939 is a potent, cell-permeablesmall molecule inhibitor of the Wnt/βcatenin pathway to TNKS1 and TNKS2with IC50 values of 11 and 4 nMrespectively.

M2237 IWP-2

IWP-2 is an inhibitor of Wnt productionthat impairs Wnt pathway activity in vitrowith an IC50 value of 27 nM.

M2042 Cilengitide (EMD121974,NSC707544)

Cilengitide (EMD 121974, NSC 707544) is aselective inhibitor of αvβ3 integrin and αvβ5integrin with IC50 of 1 nM and 140 nM,respectively.

M2008 ICG-001

ICG-001 is a novel small moleculeinhibitor of TCF/beta-catenin-mediated transcription.

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PI3K InhibitorsWnt/beta-catenin Inhibitors

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Kinesin InhibitorsIntegrin Inhibitors

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M1786 Ispinesib (SB-715992, CK0238273)

Ispinesib (SB 715992) is the first potent,highly specific small-molecule inhibitor ofkinesin spindle protein (KSP) with an IC50of 4.1 nM.

PI3K InhibitorsKinesin Inhibitors

M1983 SB-743921

SB-743921 is a highly potent and activeKSP 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.

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M2171 GSK923295

GSK923295 is an allosteric inhibitor of CENP-E with Ki valueof 3.2 nM.

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M1877 ZM447439

ZM447439 is the first Aurora family kinaseinhibitor with IC50 of 50 nM for Aurora Bkinase.

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 AuroraB and Aurora A respectively.

M1655 AT9283

AT9283 is a potent inhibitor of several protein kinases, includingAurora A, Aurora B, Janus kinase 2 (JAK2), JAK3, and ABL.

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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 apotent and selective pan-Aurorakinase inhibitor active against allBcr/Abl proteins.

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M2127 Hesperadin

Hesperadin is an ATP-competitiveinhibitor of Aurora B kinase withIC50 of 250 nM.

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M2103 CCT137690

CCT137690 is a potent inhibitor ofAurora kinases with IC50 values of15, 19, 25 nM at Aurora A, AuroraC and Aurora B respectively.

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M1706 ENMD-2076

ENMD-2076 is an orally-active, AuroraA/angiogenic kinase inhibitor.

M1691 CCT-129202

CCT129202 is an Aurora kinase inhibitorwith 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.

M1752 MLN8237 (Alisertib)

MLN8237 (Alisertib) is a second-generation,orally bioavailable, highly selective Aurorakinase A inhibitor with IC50 of 61 nM.

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PI3K InhibitorsAurora Kinase Inhibitors

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M1751 MLN8054

MLN8054 is an orally bioavailable,highly selective small moleculeinhibitor of Aurora with IC50s of0.004uM and 0.172uM. for AuroraA and Aurora B.

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M1769 PHA-739358 (Danusertib)

PHA-739358 (Danusertib) is a smallmolecule with low nanomolar activityagainst all aurora kinases (AKs) withIC50 value of 13 nM for aurora-A and79 nM for aurora-B respectively.

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PI3K InhibitorsM1796 PF-477736 (PF-0044736)

PF-477736 is a selective checkpointkinase 1(Chk1) inhibitor with Ki valuesof 0.49 nM and 47 nM for CHK1 andCHK2 respectively.

M1806 PD 0332991 (PD0332991, Palbociclib)

PD 0332991 is a highly specificinhibitor of Cdk4(IC50, 0.011micromol/L) and Cdk6 (IC50, 0.016 micromol/L).

M2154 TAK-901

TAK-901 is a novel small-molecule inhibitorof Aurora A and Aurora B with IC50 of 21nMand 15 nM.

M1800 JNJ-7706621

JNJ-7706621 is a dual cell cycleinhibitor with activity against cyclin-dependent kinases (CDK1, 2, 3, 6) with an IC50 of 3-175 nM and Aurora kinases (A and B) with anIC50 of 11-15 nM respectively.Size:


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M2169 AMG 900

AMG900 is a potent and selective,orally available small moleculeaurora kinase inhibitor.

M2188 Reversine

Reversine is a novel small moleculeATP-competitive Aurora kinaseinhibitor with IC50 of 98.5 nM forAurora B.

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M1710 Flavopiridol (Alvocidib, HMR-1275)

Flavopiridol (Alvocidib) is a pan-cdkinhibitor 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 selectiveATP-competitive CDK inhibitor.

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PI3K InhibitorsCDK Inhibitors

M1653 AT7519

AT7519 is a novel small molecule multi-cyclin-dependent (CDK) kinase inhibitor.

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M1807 SCH727965 (Dinaciclib)

SCH727965 (Dinaciclib) is a potent andselective CDK inhibitor with IC50 valuesof 1, 1, 3 and 4 nM for CDK2,CDK5,CDK1 and CDK9, respectively.

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M1810 AZD5438

AZD5438 is a novel, orally bioavailableinhibitor of cyclin-dependent kinase(CDK)1, 2 and 9 (IC50 values are 16, 6 and 20nM respectively).

M1974 Roscovitine (Seliciclib, CYC202)

Roscovitine is a potent and selectiveinhibitor of the cyclin-dependent kinasescdc2, cdk2 and cdk5.

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M1716 Gemcitabine HCL(Gemzar, LY-188011)

Gemcitabine (Gemzar, LY188011)inhibits DNA synthesis with an IC50of 0.06 µM.

M2112 LY2835219

LY2835219 is an orally available inhibitor of CDK4 and CDK6with IC50 of 2 nM and 10 nM, respectively.

M2065 SNS-032 (BMS-387032)

SNS-032 (BMS-387032) is a potent and selectiveinhibitor of CDK 9, 2 and 7 with IC50 values of 4, 38 and 62 nM respectively.

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M2322 PHA-767491 (CAY10572,PHA767491)

PHA-767491 is a potent ATP-competitivedual Cdc7/CDK9 inhibitor with IC50 of 10nM and 34 nM, respectively.

M1996 SCH 900776

SCH 900776 is a highly potent andfunctionally selective CHK1 inhibitorwith IC50 of 3 nM.

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M2325 CHIR-124

CHIR-124 is a novel and potent Chk1inhibitor with IC50 of 0.3 nM.

M2324 LY2603618 (IC-83)

LY2603618 (IC-83) is a selective Chk1inhibitor with potential anti-tumor activity.

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M2323 BMS265246

BMS265246 is a potent and selective CDKinhibitor for CDK1/cyclin B and CDK2/cyclinE with IC50 of 6 nM and 9 nM, respectively.

M2218 LEE011

LEE011 is a novel, orally available,potent and selective CDK4/6 inhibitor.

M1676 BIBR1532

BIBR1532 is a potent and selectivetelomerase inhibitorwith IC50 of 93nM.

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M1665 AZD7762

AZD7762 is a potent ATP-competitivecheckpoint kinase inhibitor with an IC50of 5 and <10 nM for CHK1 and CHK2respectively.

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M1698 Clofarabine (Clolar, Evoltra)

Clofarabine inhibits the enzymaticactivities of ribonucleotide reductase(IC50 = 65 nM) and DNA polymerase.

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PI3K InhibitorsCheckpoint Inhibitors

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PI3K InhibitorsM1856 Thiazovivin

Thiazovivin is a selective small moleculeRho-associated kinase (ROCK) inhibitorwhich significantly improves (200-fold)the efficiency of iPSC generation fromhuman fibroblasts.

M2143 MK-1775 (Seliciclib, CYC202)

MK-1775 is a potent and selectivesmall molecule Wee1 kinase inhibitorwith IC50 of 5.2 nM.

M2148 RKI-1447

RKI-1447 is a potent small molecule inhibitor of ROCK1 andROCK2 with IC50 of 14 nM and 6 nM, respectively.

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M1672 BI 2536

BI 2536 is a novel, highly selective,potent inhibitor of Polo-like kinase1 (Plk1) with an IC50 of 0.83 nM.

M1719 GSK461364

GSK461364 is a potent and selectivesmall molecule inhibitor of Polo-likekinase 1 (PLK1) with a Ki of 2.2 nM.

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M1872 Fasudil hydrochloride (HA-1077)

Fasudil hydrochloride is a potent Rho-associated kinase inhibitor with IC50of 10.7 μM.

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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).

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PI3K InhibitorsPLK Inhibitors

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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PI3K InhibitorsROCK Inhibitors

M1817 Y-27632 dihydrochloride

Y-27632 is a potent, selective inhibitorof Rho-associated protein kinases withIC50 values of 140-220 nM for ROCK1and ROCK2.

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PI3K InhibitorsWee1 Inhibitors

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M1704 Enzastaurin (LY317615)

Enzastaurin inhibits PKCβ,PKCα,PKCγand PKCε with IC50's of 0.006, 0.039,0.083 and 0.110 µM, respectively.

M2000 GW788388

GW788388 is a potent selectiveinhibitor of TGF-beta type I receptorand ALK5 with IC50 values of0.093 and 0.018 μM.

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M2081 LY2109761

LY2109761 is a novel TGF-β receptortype 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 potentPKC inhibitor with IC50 of 2.7 nM.

M2108 SB-525334

SB-525334 is a potent activin receptor-likekinase (ALK5)/ type I TGFβ-receptor kinaseinhibitor with IC50 of 14.3 nM.

M2016 LY364947 (HTS 466284)

LY364947 is a selective small moleculeinhibitor of the TGFβ type I receptorkinase with IC50 of 59 nM.

M2328 Pirfenidone

Pirfenidone inhibits TGF-β bioactivity byaffecting TGF-β2 mRNA expression andprocessing 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/Aktpathway in HUVECs.

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PI3K InhibitorsTGF-beta Inhibitors

M1980 LY2157299

LY2157299 is a novel clinically relevantTBRI (ALK5 kinase) inhibitor with IC50of 56 nM.

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PI3K InhibitorsPKC Inhibitors

M1861 CX-4945 (Silmitasertib)

CX-4945 (Silmitasertib) is a potentsmall molecule protein kinase inhibitorthat selectively binds to and inhibitsthe enzyme casein kinase II (CK2).

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M2208 Sotrastaurin (AEB071)

Sotrastaurin is an orally available pan-protein kinase C(PKC) inhibitor withpotential immunosuppressive and anti-neoplastic activities.

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PI3K InhibitorsM1742 Tubacin (Tubulin Acetylation Inducer)

Tubacin (Tubulin Acetylation Inducer) is a highly potent and reversible cell-permeable inhibitor of HDAC6 withIC50 of 0.004µM.

M1748 LBH589 (NVP-LBH589, Panobinostat)

LBH589 (Panobinostat) is a novel broad-spectrum HDAC inhibitorfor MOLT-4 and Reh cells with IC50 of 5 and 20nM, respectively.

M1747 LAQ824 (NVP-LAQ824)

LAQ824 (NVP-LAQ824) is a potent novelhistone deacetylase (HDAC) inhibitor withan IC50 of 0.032 μM.

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M1670 Belinostat (PXD101, PX105684)

Belinostat is a novel HDACinhibitor with IC50 of 27nM.

M1708 EX 527 (SEN0014196)

EX 527 is a potent and selective SIRT1class III histone deacetylase enzymeinhibitor with an IC50 of 38 nM.

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M1738 Niltubacin (MAZ-1391)

Niltubacin, as an inactive derivative ofTubacin, is a highly potent and selectivereversible cell-permeable inhibitor ofHDAC6.

M1722 CHR-3996

CHR-3996 is an orally bioavailable,second-generation hydroxamic acidbased inhibitor of HDAC with potentialantineoplastic activity.

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PI3K InhibitorsHDAC Inhibitors

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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M1730 ITF2357 (Givinostat, Gavinostat)

ITF2357 (Givinostat, Gavinostat) is a histone deacetylaseinhibitor. 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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M1753 Trichostatin A (TSA)

Trichostatin A (TSA) is a potent, reversible inhibitor of mammalianhistone deacetylase (HDAC) with IC50 value around 20 nM.

M1775 Tubastatin A hydrochloride

Tubastatin A is a potent and selective HDAC6inhibitor with IC50 values of 15 nM.

M1778 SB939 (Pracinostat)

SB939 is a novel potent andorally active histone deacetylasewith high tumor exposure andefficacy in mouse models ofcolorectal cancer.

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M2007 Romidepsin (FK228)

Romidepsin (FK228) is a structurally unique,potent HDAC1 and HDAC2 inhibitor withIC50 of 36 nM and 47 nM, respectively.

M1790 MGCD0103 (Mocetinostat)

MGCD0103 is a novel HDAC inhibitor, highly specific for classesI 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 histonedeacetylase (HDAC) inhibitor with IC50value of 0.43 to 2.7 μM.

M2101 PCI-34051

PCI-34051 is a potent HDAC 8inhibitor with IC50 of 0.01 μM.

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M2111 CUDC-907

CUDC-907 is a potent, orally-availablesmall molecule dual PI3K and HDACinhibitor.

M1876 Valproic acid sodium salt

Valproic acid (VPA) is a histone deacetylaseinhibitor which is reported to enhance centralGABAergic neurotransmission and inhibit Na+channels.

M1791 MS-275 (Entinostat, SNDX-275)

MS-275 is an inhibitor of histone deacetylases (HDACs) thatpreferentially inhibits HDAC1 (IC50 = 300 nM) over HDAC3(IC50 = 8 μM).

M2014 MC1568

MC1568 is a selective classII (IIa) histone deacetylas(HDAC II) inhibitor with IC50of 220 nM cells.

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M1993 Droxinostat

Droxinostat is a selective inhibitor ofHDAC3, HDAC6 and HDAC8 withIC50 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 potenthistone deacetylase (HDAC) inhibitor with the IC50 value of 10nM for HDAC-1.

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M2095 Resminostat (4SC-201, RAS2410)

Resminostat is a potent inhibitor ofHDACs 1, 3 and 6 [50% inhibitoryconcentration (IC50)=43-72 nmol/l]representing HDAC classes I and II.

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M2119 JNJ-26481585 (Quisinostat)

JNJ-26481585 (Quisinostat) is a novelsecond-generation class I HDAC inhibitor.

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PI3K InhibitorsM1732 BMN673 (BMN-673, LT-673)

BMN673 is a potent inhibitor of poly(ADP-ribose) polymerases (PARP)-1and -2.

M1857 LT-628

LT-628 is the racemate of BMN 673and LT-674.

M1785 INO-1001 (3-Aminobenzamide)

INO-1001 is a novel poly(ADP-ribose) polymerase(PARP) inhibitor with an IC50 of 3 nM.

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M2123 Rocilinostat (ACY-1215)

Rocilinostat(ACY-1215) is an HDAC6-selective inhibitor with IC50of 5 nM.

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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.

M1639 ABT-888 (Veliparib)

ABT-888 (Veliparib) is a potent inhibitorof PARP-1 and PARP-2 with Ki valuesof 5.2nM and 2.9nM respectively.

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M2236 CI-994 (Tacedinaline, PD 123654)

CI-994 (N-acetyl dinaline, PD 123654) isa novel orally active HDAC inhibitor withIC50 of 0.57 μM for HDAC1.

M1645 AG14361

AG14361 is a novel poly (ADP-ribose)polymerase-1 inhibitor with a GI50 of 0.9 µM.

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M1858 LT-674

LT-674 inhibits PARP-1 with an IC50of 144 nM.

M1972 Iniparib (BSI-201, NSC-746045)

Iniparib is an irreversible, noncompetitiveinhibitor of PARP1 that disrupts bindingbetween PARP1 and DNA by interactingwith the DNA binding domain.

M2010 BSI-401

BSI-401 is a novel poly (ADP ribose)polymerase-1 inhibitor.

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PI3K InhibitorsPARP Inhibitors

M1644 AG-014699 (PF-01367338, Rucaparib)

AG-014699 (PF-01367338, Rucaparib)is a PARP inhibitor with a Ki of 1.4 nM.

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M2056 PJ34 hydrochloride

PJ34 is a novel potent inhibitorof poly(ADP-ribose) polymerase(PARP) with EC50 of 20 nM.

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M2216 Dacarbazine (Imidazole Carboxamide)

Dacarbazine is a triazine antineoplasticagent that is used for DNA methylationvia formation of methyl adducts.

PI3K InhibitorsDNA/RNA Synthesis Inhibitors

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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 inhibitorby binding to DNA and interfering withthe cell's repair mechanism.

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M2289 Adrucil (5-FU, Carac, Efudex)

Adrucil(Fluorouracil) belongs to the familyof drugs called antimetabolites.

M2047 VE-821

VE-821 is a highly selective and potentATR inhibitor with IC50 of 26 nM.

M1801 KU-55933

KU-55933 is a cell-permeable ATP-competitive inhibitor of ATM (IC50= 13 nM; Ki = 2.2 nM)with selectivityover other PIKK family kinases (IC50= 2.5, 9.3, 16.6 μM for DNAPK, mTOR,PI 3-K, respectively; IC50 > 100 μMfor PI 4-K and ATR).

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M2187 ETP-46464

ETP-46464 is a potent inhibitor againstmTOR, ATR, DNA-PK, PI3-Kα and ATMwith IC50 of 0.6, 14, 36, 170 and 545nM,respectively.

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M2215 MK-4827 (Niraparib)

MK-4827 is a novel potent, orallybioavailable PARP-1 and PARP-2inhibitor with IC50 of 3.8 and 2.1nM,respectively.

M2224 Raltitrexed

Raltitrexed is an inhibitor ofthymidylate synthase usedin cancer chemotherapy.

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M2291 Azacitidine (5-azacytidine, Mylosar)

Azacitidine is a nucleoside analogue ofcytidine that specifically inhibits DNAmethylation by trapping DNA methyl-transferases.

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PI3K InhibitorsATM/ATR Inhibitors

M2309 CP-466722

CP-466722 is an potent and reversibleATM inhibitor.

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M2223 Cisplatin (Cisplatinum)

Cisplatin is a potent anticancer agentthat blocks DNA synthesis.

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M2290 Oxaliplatin (Eloxatin)

Oxaliplatin inhibits DNA synthesis byconforming DNA adducts.

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PI3K InhibitorsM2001 Idarubicin

Idarubicin is an anthracycline antibioticand a DNA topoisomerase II (topo II)inhibitor for MCF-7 cells.

M2089 Irinotecan hydrochloride trihydrate

Irinotecan hydrochloride trihydrate is a potent inhibitor of DNAtopoisomerase I.

M2057 Dexrazoxane HCL (Cardioxane)

Dexrazoxane hydrochloride is aTopoisomerase II inhibitor andintracellular ion chelator.

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M2292 Cytarabine

Cytarabine (Cytosine arabinoside, AraC) isan antimetabolic agent and DNA synthesisinhibitor with IC50 of 16 nM.

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M1982 Amonafide (AS1413, Quinamed)

Amonafide is a unique ATP-independentTopo II inhibitor that is being studied in thetreatment of cancer.

M2327 Daunorubicin HCL (Daunomycin HCL)

Daunorubicin HCl inhibits both DNAand RNA synthesis and inhibits DNAsynthesis with Ki of 0.02 μM.

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M2292 CX-5461

CX-5461 selectively inhibits PolI-driven transcription of rRNAwith IC50 of 142 nM in HCT-116 cells.

M1969 Doxorubicin (Adriamycin, Rubex)

Doxorubicin is an anthracycline antibiotic that inhibits DNA topoisomerase II usedin cancer chemotherapy.

M2144 Topotecan HCL (NSC 609669)

Topotecan hydrochloride is atopoisomerase I inhibitor andan apoptosis inducer.

M2199 Camptothecin

Camptothecin is a cytotoxic quinolinealkaloid which inhibits the DNA enzymetopoisomerase I (topo I).

M2217 Mitoxantrone dihydrochloride

Mitoxantrone dihydrochloride is apotent inhibitor of topoisomerase II.

PI3K InhibitorsDNA-PK Inhibitors

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M2326 Etoposide (Vepesid)

Etoposide is a semisynthetic derivativeof podophyllotoxin, which inhibits DNAsynthesis via topoisomerase II inhibitionactivity.

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M2308 NU7026

NU7026 is a DNA-PK inhibitor with IC50of 0.23 μM.

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PI3K InhibitorsTopoisomerase Inhibitors

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PI3K

/Akt/m

TOR

Epigenetics


Epig

enet

ics

M2167 (+)-JQ1

(+)-JQ1 is a potent, high affinity, selectiveBET bromodomain inhibitor.

M2024 BIX 01294

BIX 01294 is a potent inhitor of G9ahistone methyltransferase with IC50of 2.7 μM.

M2179 EPZ-5676

EPZ-5676 is a potent and selectiveaminonucleoside inhibitor of DOT1Lhistone methyltransferase.

M2182 RG108

RG108 is a novel small-molecule inhibitorsof DNA methyltransferases with IC50 of 115nM.

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M1824 SRT1720

SRT1720 is a selective small moleculeactivator of SIRT1 that is 1,000-foldmore potent than resveratrol (EC1.5= 0.16 versus 46.2 µM,respectively).

M2219 RVX-208

RVX-208 is a first-in-class, smallmolecule inhibitor of BET bromodomain with IC50 of 0.51 μM forBD2.

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PI3K InhibitorsHistone demethylases Inhibitors

M2096 GSK1210151A (I-BET151)

GSK1210151A (I-BET151) is an inhibitorof the BET family with IC50 of 0.5 μM, 0.25μM and 0.79 μM for BRD2, BRD3 andBRD4, respectively.

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M2190 I-BET-762 (GSK525762)

I-BET-762 (GSK525762) is a selectivesmall molecule BET inhibitor.

M2334 EPZ004777

EPZ004777 is a potent, selective, small-molecule inhibitor of DOT1L with IC50of 0.4 nM.

PI3K InhibitorsSirtuin Inhibitors

M2275 JIB-04

JIB-04 is a selective inhibitor of Jumonjihistone demethylase with IC50 values of230, 340, 435, 445, 855 and 1100 nMfor JARID1A, JMJD2E, JMJD2B, JMJD2A,JMJD3 and JMJD2C respectively.

PI3K InhibitorsDNA Methyltransferase Inhibitors

M2052 Decitabine (NSC 127716)

Decitabine is a potent inhibitor of DNAmethylation for the treatment of myelody-splastic syndromes.

PI3K InhibitorsEpigenetic Reader Domain Inhibitors

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PI3K InhibitorsHistone Methyltransferase Inhibitors

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NF-κB


NF-κB

PI3K Inhibitors

M2040 Bay 11-7082 (Bay 11-7821)

Bay 11-7082 is an inhibitor of cytokine-induced IκB-α phosphorylation (IC50~ 10 μM).

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M1812 GANT58 (Adriamycin, Rubex)

GANT58 is a cell-permeable GLI antagonistthat inhibits GLI1-induced transcription (IC50= 5 μM).

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M1713 GDC-0449 (Vismodegib, HhAntag691)

GDC-0449 (Vismodegib) is a potent,specific hedgehog pathway inhibitorwith IC50 values of 1.4 and 3.0μMfor inhibition of ABCG2 and Pgprespectively.

M2110 LY2940680

LY2940680 is a potent Hedgehog inhibitorwith potential anticancer activity.

M2300 TPCA-1 (Niraparib)

TPCA-1 is an inhibitor of IKK-2 withIC50 of 17.9 nM.

M2336 BMS-345541 hydrochloride

BMS-345541 hydrochloride is a selectiveinhibitor of the catalytic subunits of IKK(IC50 values of 0.3 μM and 4 μM forIKK-2 and IKK-1 respectively).

M2197 Sulfasalazine (Salazopyrin)

Sulfasalazine is an inhibitor of NF-κBactivation and a prodrug of the anti-inflammatory agent 5-aminosalicylicacid.

M2298 QNZ (EVP4593)

QNZ is an inhibitor of NF-κB activationwith IC50 of 11 nM.

M1874 Purmorphamine

Purmorphamine is a small molecule Hhagonist which activates the hedgehogpathway by directly binding to SMO.

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Stem Cells & Wnt

PI3K InhibitorsHedgehog Inhibitors

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M1975 Cyclopamine

Cyclopamine is a naturally occuring steroidalalkaloid that causes cyclopia by blocking sonichedgehog signaling.

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IκB/IKKrsIκB/IKK Inhibitors

M2060 SC-514 (GK 01140)

SC-514 is a selective and reversibleinhibitor of IκB kinase 2 (IKK2) withIC50 of 3-12 μM.

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IκB/IKKrsNF-κB Inhibitors

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HOT

NEW

NEW

NEW

PI3K

/Akt/m

TOR

Neuronal Signaling


Neu

rona

l Sig

nalin

g

M2231 Dimebon dihydrochloride

Dimebon dihydrochloride is a non-selective antihistamine that displayscognitive enhancing abilities.

M2279 Citalopram HCL (Celexa, Cipramil)

Citalopram (Celexa, Cipramil) is anantidepressant drug.

M1830 Firocoxib

Firocoxib is a selective COX-2 inhibitorexhibiting high selectivity to inhibit COX-2.

M2146 Prucalopride

Prucalopride is a potent, selectiveand specific serotonin 5-HT4 receptoragonist with enterokinetic properties.

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M1930 Granisetron hydrochloride

Granisetron hydrochloride is a potentand selective 5-HT3 receptor antagonistthat possesses potent antiemetic activity.

M2263 Ondansetron HCL (GR 38032, SN 307)

Ondansetron hydrochloride is a5-HT3 receptor antagonist withKi of 6.16 nM.

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M2175 Palonosetron hydrochloride

Palonosetron hydrochloride is a novelantiemetic 5-HT3-receptor antagonist.

M2262 Mianserin hydrochloride (Bolvidon)

Mianserin hydrochloride is a non-selectivE5-HT2 receptor antagonist.

M1965 Celecoxib (Celebrex, Celebra)

Celecoxib is a selective COX-2 inhibitor(IC50 values are 15 and 0.04μM for COX1 and COX-2 respectively).

PI3K Inhibitors5-HT Receptor 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 receptorantagonist, a 5-HT1B receptor partialagonist, a 5-HT1A receptor agonist and a 5-HT transporter (5-HTT) inhibitor in vitro.

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PI3K InhibitorsCOX Inhibitors

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M2131 SB-269970 HCL(SB269970A)

SB-269970 hydrochloride is a potent andselective 5-HT7 receptor antagonist withpKi of 8.3.

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M2230 Agomelatine (Valdoxan, Melitor)

Agomelatine is a metabolically stable analogof melatonin that displays agonist activity forMT1 and MT2 binding with nanomolar affinity.

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M2233 Nepafenac

Nepafenac is an analgesic selectiveinhibitor of COX-2.

Neuronal Signaling


Neuronal Signaling

PI3K Inhibitors M2130 LY-411575 (LSN-411575)

LY-411575 is potent and selectivesmall molecule γ-secretase inhibitorwith IC50 of 0.1 nM for APP23 andAPP51/16 primary neurons.

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M2069 Mirabegron (YM-178)

Mirabegron (YM178) is a potent and selective β(3)-adrenoceptoragonist with EC50 of 22.4 nM.

PI3K InhibitorsAdrenergic Receptor Inhibitors

M2172 LY2811376

LY2811376 is an orally available, non-peptidic β-secretase inhibitor with IC50of 239 nM-249 nM.

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IκB/IKKrsGamma-secretase Inhibitors

M1987 LY2886721

LY2886721 is an orally-available, furothiazine-based inhibitor of b-amyloid protein cleavingenzyme (BACE).

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IκB/IKKrsBACE Inhibitors

M1947 BMS-708163 (Avagacestat)

BMS-708163 (Avagacestat) is a selectiveγ-secretase inhibitor (IC50 = 0.3 nM).

M1746 DAPT (GSI-IX)

DAPT (GSI-IX) is a γ-secretase inhibitor with IC50 values of115 and 200 nM for total Aβ and Aβ42 respectively.

M2015 RO4929097

RO4929097 is a potent and selectiveinhibitor of γ-secretase and as a resultis able to inhibit Notch pathwaysignaling.

M1893 Etomidate (Amidate, R16659)

Etomidate (marketed as Amidate) is aanesthetic with GABA modulatory andGABA-mimetic actions.

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M1891 SKF 89976A hydrochloride

SKF 89976A hydrochloride is a potentGABA uptake inhibitor, selective forGAT-1.

IκB/IKKrsGABA Receptor Inhibitors

M2005 (R)-baclofen (STX 209)

(R)-baclofen is a selective gamma-aminobutyricacid(B) agonist.

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M2120 MK-0752

MK-0752 is a potent, oral inhibitor ofγ-secretase with IC50 of 5 nM in humanSH-SY5Y cells.

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IκB/IKKrsGluR Receptor Inhibitors

M1926 LY404039

LY404039 is a potent agonist of recombinanthuman mGlu2, mGlu3 receptors with Ki of149 nM, 92 nM respectively.

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HOT

HOT

NEW

NEW

PI3K

/Akt/m

TOR

Neuronal Signaling


Neu

rona

l Sig

nalin

g

M2051 CP 945598 HCL (Otenabant HCl)

CP 945598 hydrochloride is a selectiveand high affinity CB1 antagonist (Ki valuesare 0.7 and 0.12 nM in binding andfunctional assays respectively).

M1898 Plerixafor (AMD3100)

Plerixafor (AMD3100) is a CXCR4chemokine receptor antagonist.

M2214 JTC-801

JTC-801 is a novel opioid receptor-like1(ORL1) receptor antagonist with IC50 of94 nM.

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M2088 Ciproxifan maleate

Ciproxifan is an orally bioavailable,extremely potent histamine H3 inverseagonist/antagonist.

M2012 AM1241

AM1241 is a cannabinoid CB2 receptorselective agonist.

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M1907 Org 27569

Org 27569 is a potent and selectiveallosteric modulator ofthe cannabinoid CB1 receptor.

M2041 WZ811

WZ 811 is a potent CXCR4 antagonist (EC50 = 0.3 nM).

PI3K InhibitorsHistamine Receptor Inhibitors

PI3K InhibitorsP2 Receptor Inhibitors

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M1953 ADL5859 Hydrochloride

ADL5859 is a potent, selective and orally\bioavailable δ-opioid receptor agonist (Ki= 0.84 nM, EC50 = 20 nM).

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M2234 Prasugrel (Effient, Efient)

Prasugrel is a platelet inhibitor irreversiblybinding to P2Y12 receptors.

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M2161 SCH527123

SCH527123 is a novel, selectiveCXCR2 receptor antagonist withIC50 of 3 nM.

PI3K InhibitorsOpioid Receptor Inhibitors

M1909 GW 791343 hydrochloride

GW 791343 hydrochloride is a non-competitive inhibitor ofhuman P2X(7) receptor

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GPCR & G Protein

PI3K InhibitorsCannabinoid Inhibitors

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PI3K InhibitorsCXCR Inhibitors

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NEW

GPCR & G Protein


GPC

R &

G Protein

PI3K Inhibitors M2124 MK-6096

MK-6096 is an orally bioavailablepotent and selective reversibleantagonist of OX(1)R and OX(2)R.

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M1816 Zibotentan (ZD4054)

Zibotentan (ZD4054) is a more selectiveand specific endothelin-A receptor (ETAR)antagonist with an IC50 value of 21 nM.

PI3K InhibitorsEndothelin Receptor Inhibitors

M2272 Suvorexant (MK-4305)

Suvorexant (MK-4305) is a potent,selective and orally bioavailableantagonist of OX(1)R and OX(2)Rfor the treatment of insomnia.

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IκB/IKKrsOX Receptor Inhibitors

M1951 Ambrisentan

Ambrisentan is an orally active, highly selectiveantagonist of the endothelin-1 type A receptor.

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M2205 Macitentan (ACT-064992)

Macitentan is an orally-active, tissuetargeting dual ET receptor antagonist.

M2029 Sitaxsentan sodium (TBC-11251)

Sitaxsentan (TBC-11251) is an orally active,highly selective antagonist of endothelin Areceptors.

M2278 Bosentan Hydrate

Bosentan is an endothelin eceptorsantagonist for ET-A and ET-B with Kiof 4.7 nM and 95 nM, respectively.

M2002 Canagliflozin

Canagliflozin is a potent, selectivesodium glucose co-transporter 2 inhibitor.

M1937 Dapagliflozin (BMS-512148)

Dapagliflozin is a selective, orallyactive inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2).

IκB/IKKrsSGLT Inhibitors

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M1711 Febuxostat (Uloric, TMX-67)

Febuxostat (Uloric) is a non-purineselective xanthine oxidase inhibitorwith IC50 of 114 -210 nM.

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NEW

NEW

PI3K

/Akt/m

TOR

Endocrinology & Hormones


Endo

crin

olog

y &

Hor

mon

es

M2020 GW9508

GW9508 is a small-molecule agonist of thefatty acid receptors GPR40 and GPR120.

M2091 OC000459

OC000459 is a potent, selective, andorally active D prostanoid receptor 2antagonist.

M1986 Andarine (GTx-007, S-4)

Andarine (GTx-007, S-4) is an orally active partial agonistfor androgen receptors.

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M1960 Bicalutamide (Casodex, Cosudex)

Bicalutamide is an orally activenon-steroidal androgen receptorantagonist (IC50 = 190 nM).

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M2097 LY500307 (Erteberel)

LY500307 is a potent, selective estrogenreceptor beta agonist with an EC50 of 0.66 nM.

PI3K InhibitorsAndrogen Receptor Inhibitors

M1973 Ostarine (GTx-024,MK-2866)

Ostarine (GTx-024,MK-2866) isan investigational selective androgenreceptor modulator (SARM) withKi of 3.8 nM.

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M2270 ARN-509

ARN-509 is a novel androgenreceptor (AR) antagonist for thetreatment of castration-resistantprostate cancer (CRPC).

M2092 AZD3514

AZD3514 is a potent, small-molecule androgen receptordownregulator with potential anticancer cancer activity.

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PI3K InhibitorsEstrogen Receptor Inhibitors

M1966 Fulvestrant (Faslodex)

Fulvestrant (Faslodex) is a novel estrogen receptor antagonist(IC50 = 0.29 nM).

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PI3K InhibitorsGPR Inhibitors

M2054 TAK-875

TAK-875 is a novel, orally available, selective GPR40 agonist.

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HOT

NEW

Transmembrane Transporters


Transmem

brane Transporters

PI3K Inhibitors

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M1997 Oligomycin A (BRN 5702132, RP-32705)

Oligomycin A is an inhibitor of mitochondrialATP synthase and uncoupler of oxidativephosphorylation.

PI3K InhibitorsATPase Inhibitors

M1845 LY335979 (Zosuquidar trihydrochloride)

LY335979 (Zosuquidar trihydrochloride)is a selective Pgp(P-glycoprotein) inhibitorwith a Ki of 59 nM.

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M2294 Brefeldin A (BFA)

Brefeldin A is a lactone antibiotic andATPase inhibitor for protein transportwith IC50 of 0.2 μM in HCT 116 cells.

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M1771 PTC124 (Ataluren)

PTC124 (Ataluren) is a novel smallmolecular CFTR-G542X nonsenseallele inhibitor.

M1854 VX-770 (Ivacaftor)

VX-770 (Ivacaftor) is a potentiator of CFTR,which targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM,respectively.

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M1923 Lonidamine (AF 1890)

Lonidamine is a novel CFTR open channelblocker with an IC50 of 0.85 mM, whichinhibits aerobic glycolysis in cancer cells.

M1888 Tariquidar (XR9576)

Tariquidar (XR9576) is a selective,highly efficacious third generationP-glycoprotein (P-gp) inhibitor.

M1853 Biricodar (VX-710, Incel)

The pipecolinate derivative Biricodar(VX-710, Incel) is a clinically applicablemodulator of P-glycoprotein (Pgp)with potential chemosensitizing activity.

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IκB/IKKrsCFTR Inhibitors

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M2102 VX-809 (Lumacaftor)

VX-809 is a CFTR corrector that improves CFTR processingand maturation in the cell.

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PI3K InhibitorsP-gp Inhibitors

IκB/IKKrsPotassium Channel Inhibitors

M2043 TAK-438

TAK-438 is a novel and potentpotassium-competitive acid blocker(P-CAB) with IC50 of 19 nM.

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IκB/IKKrsSodium Channel Inhibitors

M2210 A-803467

A-803467 is a potent and selective Nav1.8 sodium channelblocker that potently blocks tetrodotoxin-resistant currents(IC50 = 140 nM).

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HOT

HOT

PI3K

/Akt/m

TOR

Metabolism


Met

abol

ism

M2206 TH-302

TH-302 is a highly potent andselective hypoxia-activatedprodrug targeting hypoxicregions of solid tumors withIC50 of 19 nM.

M2297 CPI-613

CPI-613 inhibits mitochondrial enzymespyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase.

M2142 Anacetrapib (MK-0859)

Anacetrapib is an orally active and potentinhibitor of CETP with IC50 of 7.9 nM and11.8 nM for rhCETP and mutant CET(C13S) respectively.

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M1829 Torcetrapib (CP-529414)

Torcetrapib(CP-529414) is a prototypecholesteryl ester transfer protein(CETP)inhibitor with potential for decreasingatherosclerotic disease, increasedcardiovascular events in clinical trials.

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M2058 Ketoconazole

Ketoconazole is a potent inhibitor ofcytochrome P450c17.

PI3K InhibitorsCETP Inhibitors

M1636 Abiraterone acetate (CB-7598)

Abiraterone acetate (CB-7598) is a potent,selective, and orally available inhibitor ofCYP17 with an IC50 of 4 nM.

M2330 Evacetrapib (LY2484595)

Evacetrapib (LY2484595) is a potent andselective inhibitor of CETP which inhibitedhuman recombinant CETP protein (5.5nMIC(50)) and CETP activity in human plasma(36 nM IC(50)) in vitro.

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PI3K InhibitorsCYP17 Inhibitors

M1814 Avasimibe (CI-1011)

Avasimibe (CI-1011) is a novel orallybioavailable ACAT inhibitor.

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PI3K InhibitorsDehydrogenase Inhibitors

M2067 AGI-5198 (IDH-C35)

AGI-5198 (IDH-C35) is the first highlypotent and selective inhibitor of IDH1R132H and R132C mutants in vitrowith IC50 values of 0.07 μM and 0.16μM, respectively.Size:


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M1839 MDV3100 (Enzalutamide)

MDV3100 is an orally bioavailable, organic,non-steroidal small molecule targeting theandrogen receptor (AR) with potentialantineoplastic activity.

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PI3K InhibitorsFactor Xa Inhibitors

M1649 Apixaban (BMS-562247-01)

Apixaban is a highly selective,reversibleand direct factor Xa inhibitor with anIC50 of 0.22±0.02 µM.

M1776 Rivaroxaban (Xarelto,BAY 59-7939)

Rivaroxaban (Xarelto, BAY 59-7939) is oral direct factor Xainhibitor with an IC50 value of 2.1nM.

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HOT

HOT

Metabolism


Metabolism

PI3K Inhibitors

Size:


M2126 Fluvastatin sodium

Fluvastatin sodium is an orally active,potent and competitive HMG-CoAreductase inhibitor with IC50 valuebetween 40 and 100 nM at humanliver microsomes.

PI3K InhibitorsHMG-CoA Reductase Inhibitors M1906 Piclamilast (RP 73401)

Piclamilast (RP 73401) is a potent andselective inhibitor of phosphodiesterase(PDE) 4.

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M2006 Safinamide Mesylate (FCE28073)

Safinamide is a highly selective andreversible monoamine oxidase typeB (MAO-B) inhibitor.

M1728 GSK256066

GSK256066 is a selective phosphodiesterase4 (PDE4)inhibitor with an IC50 of 3.2 pM.

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M1734 BAY-60-7550

BAY-60-7550 is a potent PDE2 inhibitorwith IC50 values of 2.0 nM (bovine) and4.7 nM (human).

M2286 Sildenafil citrate

Sildenafil citrate is an agent used totreat erectile dysfunction and pulmonaryarterial hypertension (PAH).

M2030 Apremilast (CC-10004)

Apremilast is a novel, orally available smallmolecule inhibitor of PDE4 with IC50 of 74nM.

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IκB/IKKrsMonoamine Oxidase Inhibitors

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M1871 Roflumilast (Daxas, Daliresp)

Roflumilast(Daxas,Daliresp) is a noveland selective, long-acting inhibitor ofphosphodiesterase 4 (PDE-4).

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IκB/IKKrsPPAR Inhibitors

M1880 WY 14643 (Pirinixic Acid)

WY 14643 (Pirinixic Acid) is a potentand selective, peroxisome proliferatoractivated receptor-α (PPARα) agonist.

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M2033 GSK3787

GSK3787 is an orally availableselective peroxisome proliferator-activated receptor δ (PPARδ)antagonist (pIC50 = 6.6).

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IκB/IKKrsPDE Inhibitors

M1894 Rosiglitazone (BRL 49653)

Rosiglitazone is a selective ligandof peroxisome proliferator-activatedreceptor gamma (PPARgamma).

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HOT

HOT

PI3K

/Akt/m

TOR

Metabolism


Prot

ease

s

M1883 Ubenimex (Bestatin)

Ubenimex, also known as bestatin,is a competitive protease inhibitor.

M2200 Ciprofibrate (Erteberel)

Ciprofibrate is a peroxisome proliferator-activated receptor α (PPARα) agonist.

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M2038 Rosiglitazone maleate (Avandia)

Rosiglitazone maleate (Avandia) isa potent and selective PPARγ ligandthat binds to the PPARγ ligand-binding domain with a Kd valueof 43 nM.

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M2059 A-922500

A-922500 is a potent and selective DGAT-1 inhibitor with IC50values of 7 and 24nM at human and mouse DGAT-1 respectively.

M1885 Tipifarnib (R115777)

Tipifarnib (R115777) is an oral farnesyltransferase inhibitor with activity in AML.

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M2287 APO866 (FK866)

APO866 effectively inhibits NAMPTwith IC50 of 0.09 nM.

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PI3K InhibitorsTransferase Inhibitors

M2196 P22077

P22077 is a selective inhibitor of ubiquitin-specific protease (USP) 7 with EC50 of 8.6 μM.

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M2307 Lonafarnib (SCH 66336)

Lonafarnib (SCH 66336) is a selectivelyFPTase inhibitor for H-ras, K-ras-4Band N-ras with IC50 of 1.9 nM, 5.2nMand 2.8 nM, respectively.

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PI3K InhibitorsDPP-4 Inhibitors

M1967 Sitagliptin phosphate monohydrate

Sitagliptin phosphate (MK-0431) is apotent inhibitor of dipeptidyl peptidase-4 (DPP-4) with IC50 of 19 nM.

M2277 Semagacestat (LY450139)

Semagacestat (LY450139) is a γ-secretaseblocker for Aβ42, Aβ40 and Aβ38 with IC50of 10.9 nM, 12.1nM and 12.0 nM, respectively.

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Proteases

PI3K InhibitorsAminopeptidase Inhibitors

PI3K InhibitorsDeubiquitinase Inhibitors

M2195 P5091

P5091 is a potent and selective inhibitorof ubiquitin-specific protease(USP) 7 withIC50 of 4.2 μM.

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PI3K InhibitorsGamma-secretase Inhibitors

HOT

HOT

Proteases


Proteases

PI3K Inhibitors

M1808 Telaprevir (VX-950)

Telaprevir (VX-950) is a novel hepatitis C virus (HCV) NS3-4Aprotease inhibitor with IC50 of < 0.2 μM.

PI3K InhibitorsHCV Protease Inhibitors M2035 IU1

IU1 is a reversible, small molecule inhibitorof deubiquitination by USP14 that demonstratesan IC50 value of 4-5 μM.

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M1843 BMS-790052

BMS-790052 is a first-in-class, nonstructural protein 5A(NS5A)replication complex inhibitor with an EC50 of 9-50 pM.

M2333 ABT-333

ABT-333 is a nonnucleoside NS5Bpolymerase inhibitor for the treatmentof HCV infection.

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M1686 Bortezomib (Velcade)

Bortezomib (Velcade) is a highly selectiveproteasome inhibitor with a ki value of 6 nM.

M2122 MLN9708

MLN9708 is a novel orally bioactiveproteasome inhibitor.

M2071 ONX-0914 (PR-957)

ONX-0914 (PR-957) is a potent and selectiveimmunoproteasome inhibitor.

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M1844 ITMN-191 (Danoprevir, RG7227)

ITMN-191 (Danoprevir,RG7227) is apotent and orally active inhibitor ofhepatitis C virus (HCV) NS3/4A serineprotease with an IC50 of 1.6 nM.

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M2152 Carfilzomib (PR-171)

Carfilzomib (PR-171) is a novel and selective, irreversibleproteasome inhibitor with IC50 of <5 nM.

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M2150 Oprozomib (ONX 0912, PR-047)

Oprozomib (ONX 0912) is a novelorally proteasome inhibitor withpotential antineoplastic activity.

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IκB/IKKrsProteasome Inhibitors

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M1902 MG132

MG132 is a specific and potent cell-permeable proteasomeinhibitor (IC50 = 100 nM, Ki = 4 nM).

M2141 Aclacinomycin A (Aclarubicin)

Aclacinomycin A (aclarubicin) is ananthracycline anticancer agent withdemonstrated activity against bothleukemias and solid tumors.

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HOT

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M1971 Maraviroc (Selzentry,UK-427857)

Maraviroc (UK-427857) is a selectiveCCR5 antagonist with potent anti-humanimmunodeficiency virus type 1 (HIV-1)activity and favorable pharmacologicalproperties.

M2285 MLN2238

MLN2238 inhibits the chymotrypsin-likeproteolytic (β5) site of the 20S proteasomewith IC50 and Ki of 3.4 nM and 0.93 nM,respectively.

M2193 Epoxomicin (BU 4061T)

Epoxomicin is a cell-permeable,novel proteasome inhibitor withan IC50 value of 4 nM.

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M2156 MK-0812

MK-0812 is a potent and selective CCR2antagonist with low nM affinity for CCR2on human monocytes.

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PI3K InhibitorsHIV Protease Inhibitors

M1657 Atazanavir Sulfate (BMS-232632)

Atazanavir sulfate (BMS-232632, Reyataz) is an azapeptideinhibitor of HIV-1 protease.

M2158 Lopinavir (ABT-378)

Lopinavir (ABT-378) is a potentprotease inhibitor.

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Microbiology

PI3K InhibitorsCCR Inhibitors

M2032 Vicriviroc Malate (SCH 417690)

Vicriviroc (SCH 417690) is a pyrimidine CCR5entry inhibitor of HIV-1 with IC50 of 0.91 nM.

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Microbiology


Microbiology

PI3K InhibitorsM2159 Ritonavir (ABT-538)

Ritonavir (ABT-538) is an HIVprotease inhibitor used frequentlyas a booster of other proteaseinhbitors.

PI3K InhibitorsIntegrase Inhibitors

M1681 BMS-707035

BMS-707035 is an HIV-1 integrase(IN) inhibitor. HIV-1 integrase (IN)represents a therapeuticallyadvantageous viral target to treatHIV/AIDS in the clinic.

M1718 S/GSK1349572 (Dolutegravir)

S/GSK1349572 (Dolutegravir) is a novel integrase inhibitorwith an IC50 of 2.7 nM.

M2106 Azilsartan (TAK-536)

Azilsartan (TAK-536) is an angiotensinII type 1 (AT1) receptor antagonist withIC50 of 2.6 nM.

M2105 Azilsartan medoxomil (TAK-491)

Azilsartan medoxomil is an orallyadministered angiotensin II receptortype 1 antagonist.

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M2137 Stavudine (D4T)

Stavudine (D4T) is a potent inhibitor of HIV-1reverse transcriptase in vitro.

M2258 Losartan potassium

Losartan potassium is a selective non-peptide angiotensin AT1 receptorantagonist.

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M2164 PD 123319 ditrifluoroacetate

PD123319 ditrifluoroacetate isa potent, selective, non-peptideangiotensin AT2 receptor antagonist.

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M1979 Elvitegravir (EVG)

Elvitegravir (EVG) is a HIV integraseinhibitor with IC50 of 0.7 nM, 2.8 nMand 1.4 nM for HIV-1 IIIB, HIV-2 EHOand HIV-2 ROD, respectively.

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PI3K InhibitorsReverse Transcriptase Inhibitors

PI3K InhibitorsAngiotensin Receptor Inhibitors

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PI3K InhibitorsAutophagy Inhibitors

M1834 Omeprazol (Omeprazole)

Omeprazol is a proton pump inhibitorused in the treatment of dyspepsia, laryngopharyngeal reflux (LPR) andZollinger–Ellison syndrome.

M2129 Temozolomide (NSC362856)

Temozolomide is an oral DNA methylating,chemotherapeutic agent.

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M1836 Deslorelin

Deslorelin is an injectable gonadotropin releasing hormonesuper-agonist(GnRH agonist) also known as an LHRH agonist.M2133 MK-3207 hydrochloride

MK-3207 hydrochloride is a potentCGRP receptor antagonist withIC50 of 0.12 nM.

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M2204 T0901317

T0901317 is a potent and selectiveagonist for both LXRα and LXRβ withan EC50 of ~ 50 nM.

M2265 Pirarubicin (THP-Adriamycin)

Pirarubicin is an anti-neoplastic and inhibitor of Topo II.

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PI3K InhibitorsFarnesoid X Receptor Inhibitors

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PI3K InhibitorsCGRP Receptor Inhibitors

M2018 GW4064

GW4064 is a selective, non-steroidal agonist of the orphannuclear receptor FXR with EC50 of 15 nM.

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M2165 WAY-362450 (XL335)

WAY-362450 (XL335) is a potent,selective, and orally bioavailableFXR agonist with EC50 of 4 nM.

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PI3K InhibitorsLHRH/GnRH Inhibitors

M1835 Goserelin

Goserelin is an injectable gonadotropinreleasing hormone superagonist (GnRHagonist), also known as a luteinizinghormone releasing hormone (LHRH)agonist.

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M1929 GW3965 hydrochloride

GW3965 hydrochloride is a selective, orally active non-steroidalsynthetic liver X receptor (LXR) agonist.

PI3K InhibitorsLiver X Receptor Inhibitors

PI3K InhibitorsTopoisomerase Inhibitors

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Others


Others

PI3K Inhibitors

M1729 H-89 Dihydrochloride

H-89 is a selective inhibitor ofprotein kinase A (PKA) with anIC50 value of 135 nM.

PI3K InhibitorsTRPV Inhibitors

M1846 SB-705498

SB-705498 is a potent, selective and orally bioavailable transientreceptor potential vanilloid 1 (TRPV1) receptor antagonist with apIC50 of 7.1.

M1707 Entecavir Monohydrate (Baraclude)

Entecavir Monohydrate (Baraclude) inhibitsreverse transcription, DNA replication andtranscription with an IC50 of 0.5 nM.

M1695 Cidofovir (Vistide)

Cidofovir (Vistide) is an injectable antiviral medication for the treatmentof cytomegalovirus (CMV) retinitis.

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M1674 BIBR 953 (Dabigatran, Pradaxa)

BIBR 953 (Dabigatran, Pradaxa) is an oral anticoagulant fromthe class of the direct thrombin inhibitors.

M1797 Retigabine (D2312, D-23129)

Retigabine is a KCNQ/Kv7 potassiumchannel activator which functions byenhancing potassium currents viastabilizing the open conformation ofthe Kv7.2-7.3 channels.

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M1737 MF63

MF63 is a selective mPGES-1 inhibitorwith an IC50 of 0.9 nM and 1.3 nM forpig mPGES-1 and human mPGES-1enzyme respectively.

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M1650 Aprepitant (MK-0869, L-754030)

Aprepitant (Emend) is an antiemeticchemical compound that belongs toa class of drugs called substance Pantagonists (SPA).

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M1803 Laquinimod (ABR-215062)

Laquinimod (ABR-215062) is a neworally active immunoregulator effectivelyinhibits development and relapses ofexperimental autoimmune encephalomyelitis.

M1831 Cyclosporine A (Cyclosporine)

Cyclosporine A is a powerful immunosuppressive agent thatinhibits the T-cell receptor signal transduction pathway.

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PI3K InhibitorsPKA Inhibitors

PI3K InhibitorsOther Inhibitors

M1689 BTZ043 (BTZ038, BTZ044)

BTZ043 (BTZ038, BTZ044) is adecaprenylphosphoryl-b-D-ribose2-epimerase inhibitor.

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Others


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M1895 Prasugrel hydrochloride

Prasugrel hydrochloride is a novelinhibitor of platelet activation andaggregation.

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M1911 NPI-2358 (Plinabulin)

NPI-2358 is a novel vascular disruptingagent (VDA) with an IC50 of 15 nM.

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M1910 Nepicastat hydrochloride (SYN117)

Nepicastat hydrochloride is a potentand selective inhibitor of both bovineand human dopamine-β-hydroxylasewith IC50 of 8.5 nM and 9 nM, respectively.

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M1833 Imidaclopride (Imidacloprid)

Imidaclopride is a systemic insecticidewhich acts as an insect neurotoxin andbelongs to a class of chemicals calledthe neonicotinoids.

M1864 SYN115

SYN115 is a novel, selectiveadenosine A receptor antagonist.

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M1865 Bevirimat (BVM, MPC-4326, PA-457)

Bevirimat (BVM), also known as PA-457 orMPC-4326, is a novel Human ImmunodeficiencyVirus type 1 (HIV-1) maturation inhibitor.

M1832 Maropitant (Cerenia)

Maropitant (Cerenia) is a novel, selectiveneurokinin type-1(NK1) receptor antagonist.

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M1870 Marbofloxacin

Marbofloxacin is a potent antibiotic ofthe 3rd generation fluoroquinolonegroup which inhibiting bacterial DNAreplication.

M1868 NXY-059 (Disufenton sodium,Cerovive)

NXY-059 is a free radical-trappingneuroprotectant that has been reportedto reduce infarct size and preservebrain function in experimental modelsof acute ischemic stroke.

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M1897 AZD6765

AZD6765 is an NMDA receptor antagonist.

M1903 PF-4800567

PF-4800567 is a novel and potent inhibitorof the enzyme Casein kinase 1 epsilon (IC50= 32 nM).

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M1914 Naxagolide HCL (Dopazinol HCL)

Naxagolide Hydrochloride is a potent dopamine D2-receptoragonist.

M1915 Naxagolide (Dopazinol)

Naxagolide (Dopazinol) is a very potentand selective D2 agonist.

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Others


Others

PI3K InhibitorsM1916 Nelarabine (Arranon, 506U78)

Nelarabine is a novel purine antimetaboliteantineoplastic agent.

M1917 Mozavaptan (OPC-31260)

Mozavaptan (OPC-31260) is a selectivevasopressin V2 receptor antagonist.

M1934 FK-506 (Tacrolimus, Fujimycin)

FK-506 is a potent, clinically-usefulimmunosuppressant in the samemolecular class as cyclosporin Aand rapamycin.

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M1924 Linezolid

Linezolid is a synthetic antibiotic.

M1938 Daptomycin (Cubicin, Dapcin)

Daptomycin is the first member of a new class of bactericidalantibiotics, the cyclic lipopeptides.

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M1939 Sulfadimethoxine (Di-Methox, Albon)

Sulfadimethoxine (trade name Di-Methox,Albon) is a sulfonamide antibiotic.M1927 KB-R7943 mesylate

KB-R7943 mesylate is a potent, selective inhibitor of the reversemode of the Na+/Ca2+ exchanger (IC50 = 0.7 mM).

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M1921 Mizoribine (Bredinin)

Mizoribine (Bredinin) is an imidazole nucleosideand an immunosuppressive agent with an IC50of approximately 100 μM.

M1928 KN-62

KN-62 is a selective, cell permeable inhibitor ofcalcium/calmodulin-dependent kinase II (CaMKII;IC50 = 900 nM).

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M1935 LY315920 (Varespladib)

LY315920 is a potent, selective inhibitorof recombinant human, group IIA,nonpancreatic secretory PLA2 (sPLA2).

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M1954 Alpidem (Ananxyl)

Alpidem is a potent antagonist ofperipheral benzodiazepine receptor(PBR).

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M1955 23-Hydroxybetulinic acid

23-Hydroxybetulinic acid is a novelanticancer substance.

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Others


Oth

ers

M2009 Teicoplanin

Teicoplanin is a glycopeptide antibiotic.

M2046 Calcifediol (Calcidiol)

Calcifediol is a prehormone that isproduced in the liver by hydroxylationof vitamin D3 (cholecalciferol) by theenzyme cholecalciferol 25-hydroxylase.Size:


M2037 Fesoterodine fumarate (Toviaz)

Fesoterodine fumarate (Toviaz) is a novelmuscarinic receptor antagonist.

M1958 Natamycin

Natamycin is an antifungal polyene macrolide that bindsspecifically to ergosterol and blocks fungal growth.

M1959 Oseltamivir (Tamiflu)

Oseltamivir is a potent and selectiveinhibitor of influenza virus neuraminidaseenzyme.

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M1963 Capecitabine (Xeloda)

Capecitabine (Xeloda, Roche) is anorally-administered chemotherapeuticagent.

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M1985 Odanacatib (MK-0822)

Odanacatib (MK-0822) is an inhibitor ofcathepsin K, an enzyme involved in boneresorption.

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M2034 Pemetrexed disodium (Alimta)

Pemetrexed disodium (Alimta) is a novel multitargeted antifolatefor TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM,respectively.

M2049 Metformin hydrochloride (Glucophage)

Metformin hydrochloride is anoral antidiabetic agent.

M2072 Zanamivir (OPC-31260)

Zanamivir is a neuraminidase inhibitorused in the treatment and prophylaxisof influenza caused by influenza A virusand influenza B virus.Size:


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M1961 Acitretin (Soriatane,Neotigason)

Acitretin (trade name Soriatane or Neotigason) is a second-generation retinoid.

M2004 Omecamtiv mecarbil (CK-1827452)

Omecamtiv mecarbil (formerly CK-1827452) is a sarcomeredirected cardiac myosin activator for acute and chronic heartdisease.

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Others


Others

PI3K InhibitorsM2077 Detomidine hydrochloride (Bredinin)

Detomidine hydrochloride is a nonnarcotic,synthetic alpha-2 adrenoreceptor agonist.

M2079 Chrysin

Chrysin is a naturally occurring flavonechemically extracted from the passionflowers Passiflora caerulea.

M2098 Bindarit

Bindarit is a specific anti-inflammatory smallmolecule inhibitor of MCP-1 production.

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M2085 Tie2 kinase inhibitor

Tie2 kinase inhibitor is a potent, reversible,and ATP-binding site-targetingTie2 inhibitor with anIC50 of 250 nM. M2107 Calcium levofolinate

Calcium levofolinate is a calcium salt of folinic acid that is anadjuvant used in cancer chemotherapy.

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M2086 Ribitol (Adonitol)

Ribitol (Adonitol) is a crystalline pentosealcohol formed by the reduction of ribose.

M2082 Streptozotocin (Streptozocin, STZ)

Streptozotocin is a small molecule antibioticand a potent DNA methylating agent.

M2087 HC-030031 (Varespladib)

HC-030031 is a selective TRPA1 blocker, antagonizing TRPA1-mediated calcium influx induced by AITC and formalin (IC50 =6.2 and 5.3 μM, respectively).

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M2100 Bleomycin sulfate (Blenoxane)

Bleomycin sulfate (Blenoxane) is a glycopeptide antitumorantibiotic isolated from Streptomyces verticillus.

M2114 GSK126

GSK126 is a potent, highly selective,S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2methyltransferase activity.

M2116 ABT-492 (Delafloxacin)

ABT-492 is a new fluoroquinoloneagainst 155 aerobic and 171 anaerobicpathogens.

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M2093 Enoxacin (Cubicin, Dapcin)

Enoxacin is a small molecule inhibitor ofbinding between the B2-subunit of vacuolarH+-ATPase (V-ATPase) and microfilaments.

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Others


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ers

M2162 Praziquantel (Biltricide)

Praziquantel (Biltricide) is an anthelminticeffective against flatworms.

M2170 SVT-40776

SVT-40776 is a novel M3 muscarinicreceptor antagonist.

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M2168 Aztreonam

Aztreonam is a synthetic monocyclicbeta-lactam antibiotic.

M2139 Mycophenolate mofetil

Mycophenolate mofetil is an inhibitor of inosine monophosphatedehydrogenase (IMPDH).

M2140 Posaconazole (Noxafil)

Posaconazole is a sterol C14α demethylase inhibitor withIC50 of 0.25 nM.

M2155 (1S-cis)-Milnacipran hydrochloride

(1S-cis)-Milnacipran hydrochloride is aselective norepinephrine and serotoninreuptake inhibitor approved for themanagement of fibromyalgia.

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M2157 Apaziquone

Apaziquone is a bioreductive prodrugand a chemical analog of the olderchemotherapeutic agent mitomycin C.

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M2163 PA-824

PA-824 is an experimental anti-tuberculosis drug.

M2173 Delavirdine mesylate (U-90152)

Delavirdine mesylate is a nonnucleosidereverse transcriptase inhibitor of humanimmunodeficiency virus type 1 (HIV-1).

M2174 Calcitriol

Calcitriol is an Active metabolite ofvitamin D3 that activates the vitaminD receptor.

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M2147 GM6001 (Galardin, Ilomastat)

GM6001 (Galardin,Ilomastat) is a broadspectrum matrix metalloproteinase inhibitor.

M2160 Reboxetine mesylate

Reboxetine mesylate is a potent,selective inhibitor of noradrenalinuptake (Ki values are 1.1, 129 and> 10000 nM for rat NET, SERT andDAT respectively).

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M2176 Dexamethasone

Dexamethasone is a potent anti-inflammatoryglucocorticoid that induces the production ofphospholipase A2 inhibitory protein.

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Others


Others

PI3K InhibitorsM2181 ML133 hydrochloride

ML133 hydrochloride is a selective inhibitorof the Kir2 family of inward rectifier (IRK, KCNJ) potassium channels.

M2183 Bendamustine hydrochloride

Bendamustine hydrochloride is a DNA-alkylator with a distinct pattern of activity.

M2213 Ki16425

Ki16425 is a LPA receptor antagonist withKi values of 0.34, 6.5 and 0.93 μM for thehuman LPA1, LPA2 and LPA3 receptors,respectively.

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M2189 MLN4924

MLN4924 is a novel small molecule NAEinhibitor with IC50 of 4 nM.

M2226 Melatonin (Melatonex)

Melatonin is a hormone found naturallyin the body.

M2191 Forskolin (Coleonol)

Forskolin (Coleonol) is a cell-permeableactivator of adenylyl cyclase.

M2186 UK 383367

UK383367 is a potent and selective BMP-1(procollagen C-proteinase; PCP) inhibitor with IC50 of 44 nM.

M2198 Curcumin

Curcumin is an antitumor, anti-inflammatory and antioxidantagent.

M2221 Pimecrolimus

Pimecrolimus is an immunomodulatingagent used in the treatment of atopicdermatitis.

M2227 Imiquimod (Aldara)

Imiquimod (R837), an imidazoquinoline amineanalog to guanosine,is an immune responsemodifier with potent indirect antiviral activity.

M2228 Abitrexate (Methotrexate)

Abitrexate is an antimetabolite andantifolate agent with antineoplasticand immunosuppressant activities.

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M2203 MK-8742

MK-8742 is an investigational HCV NS5A replication complexinhibitor.

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1000mg >2000mg Inquiry

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M2222 Malotilate

Malotilate is a hepatoprotective agentused in the treatment of liver disease.

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M2244 Biperiden HCL(Akineton,NSC 170950)

Biperiden hydrochloride is a muscarinicreceptor antagonist that displays someselectivity for the M1 subtype.

M2247 Carmofur (HCFU)

Carmofur is a derivative of fluorouracil, an antimetaboliteused as an antineoplastic agent.

M2246 Bumetanide

Bumetanide is a loop diuretic thatinhibits the NKCC cotransporter.

M2229 Leflunomide (Arava)

Leflunomide is an inhibitor of dihydroorotatedehydrogenase with IC50 of 2.5 μM.

M2232 Dienogest (Natazia)

Dienogest is an orally-active semisynthetic,steroidal progestogen (or progestin).

M2241 Adapalene (CD-271; Differin)

Adapalene is a third-generation topicalretinoid primarily used in the treatmentof acne.

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M2242 Altretamine

Altretamine is an antitumor agent which alsoacts as a chemosterilant for male housefliesand other insects.

M2245 Budesonide (Rhinocort, Pulmicort)

Budesonide is a synthetic anti-inflammatory glucocorticoid thatdisplays chemopreventive activity.

M2248 Cilnidipine

Cilnidipine is a dual L- and N-type calcium channel blockerthat displays antihypertensive, sympatholytic and neuro-protective activity.

M2249 Ftorafur (Tegafur)

Ftorafur is a chemotherapeutic 5-FU prodrugused in the treatment of cancers.

M2240 Acarbose (Galardin, Ilomastat)

Acarbose is an inhibitor of intestinalα-glucosidase with IC50 of 11 nM.

M2243 Aniracetam

Aniracetam is a nootropic drug that has beenshown to selectively enhance quisqualatereceptor-mediated responses in Xenopusoocytes injected with brain mRNA and inhippocampal pyramidal cells.

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M2250 Pamidronate disodium (Aredia)

Pamidronate disodium is a nitrogencontaining bisphosphonate, used toprevent osteoporosis.

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Others


Others

PI3K InhibitorsM2251 Edaravone (MCI-186)

Edaravone is a radical scavenger andantioxidant which is able to protect againstthe effects of ischemia.

MM2253 Felbamate (Felbatol)

Felbamate is an anticonvulsant,acting as an antagonist at the NMDA-associatedglycine binding site.

M2261 Meropene (Merrem, Meronem)

Meropenem is an ultra-broad-spectruminjectable antibiotic used to treat a widevariety of infections.

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M2256 Ivermectin

Ivermectin is a positive allosteric modulator of the α7 neuronalnicotinic acetylcholine receptor and the purinergic P2X4 receptor.

M2267 Resveratrol

Resveratrol is a phytoestrogen withantitumor, antioxidant, antiplatelet,anti-inflammatory and antifungaleffects.

M2257 Levetiracetam (Keppra)

Levetiracetam is an antiepileptic thatdisplays distinctive properties fromconventional antiepileptic drugs.

M2254 Gatifloxacin (Gatiflo)

Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family.

M2259 Biapenem (L-627, LJC 10627)

Biapenem is a new parenteral carbapenemantibacterial agent with a broad spectrum ofin vitro antibacterial activity.

M2264 Oxcarbazepine (Trileptal)

Oxcarbazepine is an anticonvulsant andmood-stabilizing drug.

M2268 Rocuronium bromide

Rocuronium bromide is an aminosteroidnon-depolarizing neuromuscular blockeror muscle relaxant used in modernanaesthesia

M2269 Tigecycline (Tygacil, GAR-936)

Tigecycline is a novel glycylcycline antimicrobial for intravenoususe.M2260 Gestodene (Gestinol, SHB 331)

Gestodene is a synthetic progestin usedas a contraceptive.

M2266 Pizotifen malate (Sandomigran)

Pizotifen malate is a tricycliccompound found to be a potentinhibitor of SR-2 receptor activity.

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ers

M2335 ZLN005 (CD-271,Differin)

ZLN005 is a novel and potent smallmolecule PGC-1α transcriptionalactivator.

M2273 Clodronate disodium

Clodronate disodium is the disodium saltof a nitrogen-free bisphosphonate analogof naturally occurring pyrophosphate.

M2280 Tamoxifen Citrate

Tamoxifen Citrate is an antagonist ofthe estrogen receptor by competitiveinhibition of estrogen binding.

M2283 Rosuvastatin calcium (Crestor)

Rosuvastatin(Crestor) is a member of statins and used to treathigh cholesterol and related conditions.

M2284 Tosedostat (CHR2797)

CHR-2797 is an aminopeptidase inhibitorfor LAP, PuSA and Aminopeptidase N withIC50 of 100 nM, 150 nM and 220 nM,respectively.

M2281 Exemestane (Aromasin)

Exemestane is an aromatase inhibitor, inhibitshuman placental and rat ovarian aromatasewith IC50 of 30 nM and 40 nM, respectively.

M2332 Zileuton

Zileuton is an orally active 5-lipoxygenase(5-LOX) inhibitor that inhibits LTB4 synthesis with IC50 values of 0.56, 2.3 and 2.6 μMin dog, rat and human blood respectively.

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Product Alphabetical Index

0 - 9(+)-JQ1 ................................................. 36

(1S-cis)-Milnacipran Hydrochloride ...... 56

(R)-Baclofen ......................................... 39

17-AAG................................................. 24

17-DMAG hydrochloride....................... 24

23-Hydroxybetulinic acid ...................... 53

2-Methoxyestradiol ............................... 15

3-Methyladenine..................................... 3

AA66 ......................................................... 2

A-674563................................................ 4

A-803467.............................................. 43

A-922500.............................................. 46

Abiraterone........................................... 44

Abitrexate ............................................. 57

ABT-199 ............................................... 17

ABT-263 ............................................... 17

ABT-333 ............................................... 47

ABT-492 ............................................... 55

ABT-737 ............................................... 17

ABT-751 ............................................... 24

ABT-869 ................................................. 7

ABT-888 ............................................... 33

AC220 .................................................. 15

Acarbose .............................................. 58

Acitretin ................................................ 54

Aclacinomycin A ................................... 47

Adapalene ............................................ 58

ADL5859 Hydrochloride ....................... 40

Adrucil .................................................. 34

AEE788 .................................................. 7

AG 18 ................................................... 11

AG-014699 ........................................... 33

AG14361 .............................................. 33

AG-1478 ............................................... 12

AG490 .................................................. 19

AGI-5198 .............................................. 44

Agomelatine ......................................... 38

ALK5 Inhibitor II .................................... 13

Alpidem ................................................ 53

Altretamine ........................................... 58

AM1241 ................................................ 40

Ambrisentan ......................................... 41

AMG 900 .............................................. 27

AMG-208 .............................................. 12

AMG-458 .............................................. 12

Amonafide ............................................ 15

Aztreonam ............................................ 56

BBafetinib ............................................... 16

Baricitinib .............................................. 19

Bay 11-7082 ......................................... 37

BAY-60-7550........................................ 45

Belinostat.............................................. 31

Bendamustine hydrochloride................ 57

Bevirimat .............................................. 52

BEZ235 .................................................. 1

BGJ398 .................................................. 8

BGT226 .................................................. 1

BI 2536 ................................................. 29

BI 6727 ................................................. 29

Biapenem ............................................. 59

BIBF1120 ............................................... 7

BIBR 953 .............................................. 51

BIBR1532 ............................................. 28

BIBW2992 ............................................ 10

Bicalutamide......................................... 42

BI-D1870 ................................................ 7

BIIB021................................................. 23

Bindarit ................................................. 55

Biperiden hydrochloride........................ 58

BIRB796 ............................................... 21

Biricodar ............................................... 43

Birinapant ............................................. 18

BIX 01294............................................. 36

BIX 02189............................................. 19

BIX02188.............................................. 19

BKM120.................................................. 1

Bleomycin sulfate ................................. 55

BMN673 ............................................... 33

BMS 794833......................................... 12

BMS-265246 ........................................ 28

BMS-345541 hydrochloride.................. 37

BMS-536924 ........................................ 14

BMS-599626 ........................................ 10

BMS-707035 ........................................ 49

BMS-708163 ........................................ 39

BMS-754807 ........................................ 14

BMS-777607 ........................................ 12

BMS-790052 ........................................ 47

Bortezomib ........................................... 47

Bosentan Hydrate................................. 41

Bosutinib............................................... 15

Brefeldin A............................................ 43

Amuvatinib.............................................. 9Anacetrapib .......................................... 44Andarine ............................................... 42Aniracetam ........................................... 58AP24534............................................... 15AP26113............................................... 13Apatinib .................................................. 9Apaziquone .......................................... 56Apixaban .............................................. 44APO866................................................ 46Apremilast ............................................ 45Aprepitant ............................................. 51ARN-509............................................... 42ARQ-197 .............................................. 12ARRY-162 ............................................ 18AS605240............................................... 1AS703026............................................. 18ASC-J9 ................................................. 24ASP3026 .............................................. 14Astragaloside IV ................................... 30AT-101.................................................. 17AT13387............................................... 24AT-406.................................................. 18AT7519................................................. 27AT786................................................... 73AT9283................................................. 26Atazanavir Sulfate ................................ 48AUY922 ................................................ 23AV-951 ................................................... 7Avasimibe............................................. 44AVL-292 ............................................... 16Axitinib .................................................... 7AZ 960.................................................. 19AZ3146................................................. 25AZ628................................................... 23Azacitidine ............................................ 34AZD1152-HQPA................................... 26AZD1480 .............................................. 19AZD2014 ................................................ 6AZD2281 .............................................. 33AZD2858 ................................................ 6AZD3463 .............................................. 14

AZD3514 .............................................. 42

AZD4547 .............................................. 10

AZD5363 .............................................. 4

AZD5438 .............................................. 27

AZD6244 .............................................. 18

AZD6482 ................................................ 3

AZD6765 .............................................. 52

AZD7762 .............................................. 28

AZD8055 ................................................ 4

AZD8330 .............................................. 18AZD8931 .............................................. 10Azilsartan.............................................. 49

Brivanib .................................................. 8

Brivanib alaninate................................... 8

BSI-401 ................................................ 33

BTZ043................................................. 51

Budesonide .......................................... 58

Bumetanide .......................................... 58

BX-795 ................................................... 6

BX-912 ................................................... 7

BYL719................................................... 3

CCAL-101 ................................................. 3

Calcifediol ............................................. 54

Calcitriol................................................ 56

Calcium levofolinate ............................. 55

Camptothecin ....................................... 35

Canagliflozin ......................................... 41

Canertinib ............................................. 11

Capecitabine ........................................ 54

Carboplatin ........................................... 34

Carfilzomib ........................................... 47

Carmofur .............................................. 58

CCT-129202......................................... 26

CCT137690 .......................................... 26

Cediranib ................................................ 8

Celecoxib.............................................. 38

CEP-28122........................................... 14

CEP-32496........................................... 22

CEP-33779........................................... 20

CH5132799 ............................................ 1

CH5424802 .......................................... 13

CHIR-124 ............................................. 28

CHIR-98014 ........................................... 6

CHIR-99021 ........................................... 6

CHIR-99021 HCl .................................... 6

CHR-3996 ............................................ 31

Chrysin ................................................. 55

CI-1040................................................. 18

CI-994................................................... 33

Cidofovir ............................................... 51

Cilengitide............................................. 25

Cilnidipine............................................. 58

Ciprofibrate........................................... 46

Ciproxifan maleate ............................... 40

Cisplatin................................................ 34

Citalopram hydrobromide ..................... 38

Clodronate disodium ............................ 60

Clofarabine ........................................... 28

CNX-2006............................................. 11

CO-1686............................................... 11

CP 673451 ............................................. 9

CP 945598 hydrochloride..................... 40

ENMD-2076.......................................... 26

Enoxacin............................................... 55

Entecavir Monohydrate ........................ 51

Enzastaurin .......................................... 30

Epoxomicin ........................................... 48

EPZ004777 .......................................... 36

EPZ-5676 ............................................. 36

Erlotinib Hydrochloride ......................... 10

Etomidate ............................................. 39

Etoposide ............................................. 35

ETP-46464 ........................................... 34

Evacetrapib .......................................... 44

Everolimus.............................................. 4

EX 527.................................................. 31

Exemestane ......................................... 60

FFasudil hydrochloride ........................... 29

Febuxostat............................................ 41

Felbamate ............................................ 59

Fesoterodine fumarate ......................... 54

FG-4592 ............................................... 15

Firocoxib ............................................... 38

FK-506.................................................. 53

Flavopiridol ........................................... 27

Fludarabine .......................................... 20

Fluvastatin sodium ............................... 45

Foretinib ............................................... 12

Forskolin ............................................... 57

Fosbretabulin disodium ........................ 24

Fostamatinib disodium ......................... 16

Ftorafur ................................................. 58

FTY720................................................. 15

Fulvestrant............................................ 42

GGanetespib ........................................... 23

GANT58 ............................................... 37

Gatifloxacin........................................... 59

GDC-0032 .............................................. 3

GDC-0068 .............................................. 4

GDC-0152 ............................................ 18

GDC-0349 .............................................. 5

GDC-0449 ............................................ 37

GDC-0879 ............................................ 22

GDC-0941 .............................................. 1

GDC-0941 Bimesylate............................ 3

GDC-0980 .............................................. 1

Gefitinib ................................................ 10

Gemcitabine Hydrochloride .................. 28

Genistein .............................................. 11

CP-466722 ........................................... 34

CP-547632 ............................................. 9

CP-724714 ........................................... 10

CPI-0610 .............................................. 36

CPI-613 ................................................ 44

Crenolanib .............................................. 8

CUDC-101............................................ 31

CUDC-305............................................ 23

CUDC-907............................................ 32

Curcumin .............................................. 57

CX-4945 ............................................... 30

CX-5461 ............................................... 35

CYC116................................................ 26

Cyclopamine......................................... 37

Cyclosporine A ..................................... 51

CYT387 ................................................ 19

Cytarabine ............................................ 35

DDabrafenib............................................ 22

Dabrafenib Mesylate ............................ 22

Dacarbazine ......................................... 34

Dacomitinib........................................... 11

Dapagliflozin ......................................... 41

DAPT.................................................... 39

Daptomycin .......................................... 53

Dasatinib .............................................. 15

Daunorubicin hydrochloride.................. 35

DCC-2036 ............................................ 15

Decitabine ............................................ 36

Deforolimus ............................................ 4

Delavirdine mesylate ............................ 56

Deslorelin ............................................. 50

Detomidine hydrochloride..................... 55

Dexamethasone ................................... 56

Dexrazoxane hydrochloride...................35

Dienogest ............................................. 58

Dimebon dihydrochloride...................... 38

DMXAA................................................... 9

Docetaxel ............................................. 24

Dorsomorphin dihydrochloride ............... 7

Dovitinib.................................................. 8

Doxorubicin .......................................... 35

Droxinostat ........................................... 32

EE-3810.................................................... 9

Edaravone ............................................ 59

Elesclomol ............................................ 24

Ellagic acid ........................................... 35

Elvitegravir............................................ 49

LY294002 ............................................... 2

LY2940680 ........................................... 37

LY315920 ............................................. 53

LY335979 ............................................. 43

LY364947 ............................................. 30

LY404039 ............................................. 39

LY-411575............................................ 39

LY500307 ............................................. 42

MMacitentan............................................ 41

Malotilate .............................................. 57

Maraviroc.............................................. 48

Marbofloxacin ....................................... 52

Maropitant ............................................ 52

Masitinib ................................................. 8

MC1568................................................ 32

MDV3100 ............................................. 44

Melatonin.............................................. 57

Meropenem .......................................... 59

Metformin hydrochloride....................... 54

MF63 .................................................... 51

MG132.................................................. 47

MGCD0103 .......................................... 32

MGCD265 ............................................ 13

Mianserin hydrochloride ....................... 38

Mirabegron ........................................... 39

Mitoxantrone dihydrochloride ............... 35

Mizoribine ............................................. 53

MK-0752............................................... 39

MK-0812............................................... 48

MK-1775............................................... 29

MK-2206................................................. 4

MK-3207 hydrochloride ........................ 50

MK-4827............................................... 34

MK-6096............................................... 41

MK-8742............................................... 57

ML133 hydrochloride............................ 57

MLN2238.............................................. 48

MLN2480.............................................. 22

MLN4924.............................................. 57

MLN8054.............................................. 26

MLN8237.............................................. 26

MLN9708.............................................. 47

Motesanib Diphosphate........................ 9

Mozavaptan.......................................... 53

MS-275................................................. 32

Mubritinib .............................................. 11

Mycophenolate mofetil ......................... 56

N

ITMN-191 ............................................. 47

IU1........................................................ 47

Ivermectin ............................................. 59

IWP-2 ................................................... 25

JJNJ-26481585 ...................................... 32

JNJ-26854165 ...................................... 17

JNJ-38877605 ...................................... 12

JNJ-7706621 ........................................ 27

JNK-IN-8............................................... 23

JTC-801................................................ 40

KKB-R7943 mesylate ............................. 53

Ketoconazole........................................ 44

Ki16425 ................................................ 57

Ki8751 .................................................... 9

KN-62 ................................................... 53

KU-0063794 ........................................... 5

KU-55933 ............................................. 34

KU-60019 ............................................. 34

KW-2449 .............................................. 15

KX2-391 ............................................... 16

LLapatinib Ditosylate .............................. 10

LAQ824 ................................................ 31

Laquinimod........................................... 51

LBH589 ................................................ 31

LDK378 ................................................ 14

LDN-193189 ......................................... 13

LEE011................................................. 28

Leflunomide.......................................... 58

Lenalidomide ........................................ 17

Lenvatinib ............................................... 8

Levetiracetam....................................... 59

Linezolid ............................................... 53

Lonafarnib ............................................ 46

Lonidamine........................................... 43

Lopinavir ............................................... 48

Losartan potassium .............................. 49

LT-628 .................................................. 33

LT-674 .................................................. 33

LY2109761 ........................................... 30

LY2157299 ........................................... 30

LY2228820 ........................................... 22

LY2603618 ........................................... 28

LY2811376 ........................................... 39

LY2835219 ........................................... 28

LY2886721 ........................................... 39

Gestodene............................................ 59

GM6001................................................ 56

GNE-493 ................................................ 2

Go 6983................................................ 30

Golvatinib ............................................. 13

Goserelin .............................................. 50

Granisetron hydrochloride .................... 38

GSK 3787............................................. 46

GSK1059615.......................................... 3

GSK1120212........................................ 19

GSK1210151A ..................................... 36

GSK126................................................ 55

GSK1838705A ..................................... 13

GSK1904529A ..................................... 14

GSK2126458.......................................... 2

GSK2334470.......................................... 6

GSK256066.......................................... 45

GSK2636771.......................................... 3

GSK461364.......................................... 29

GSK690693............................................ 3

GSK923295.......................................... 25

GW 791343 hydrochloride.................... 40

GW3965 hydrochloride......................... 50

GW4064 ............................................... 50

GW788388 ........................................... 30

GW9508 ............................................... 42

HH-89 Dihydrochloride............................ 51

HC-030031 ........................................... 55

Hesperadin ........................................... 26

II-BET-762 ............................................. 36

IC87114.................................................. 2

ICG-001................................................ 25

Icotinib .................................................. 10

Idarubicin .............................................. 35

Imatinib Mesylate ................................. 15

Imidaclopride ........................................ 52

Imiquimod............................................. 57

INCB18424........................................... 19

INCB28060........................................... 13

Indirubin.................................................. 6

Iniparib.................................................. 33

INK128 ................................................... 5

INO-1001.............................................. 33

IPI-145.................................................... 3

Irinotecan Hydrochloride Trihydrate ..... 35

Ispinesib ............................................... 25

ITF2357 ................................................ 31

Prucalopride ......................................... 38

PTC124 ................................................ 43

Purmorphamine.................................... 37

QQNZ...................................................... 37

RR-406.................................................... 16

R428..................................................... 14

R547..................................................... 27

R788..................................................... 16

RAF265 ................................................ 22

Raltitrexed ............................................ 34

Rapamycin ........................................... 5

Reboxetine mesylate............................ 56

Regorafenib.......................................... 7

Resminostat ......................................... 32

Resveratrol ........................................... 59

Retigabine ............................................ 51

Reversine ............................................. 27

RG108 .................................................. 36

Ribitol ................................................... 55

Rigosertib ............................................. 29

Ritonavir ............................................... 49

Rivaroxaban ......................................... 44

RKI-1447 .............................................. 29

RO4929097 .......................................... 39

Rocilinostat ........................................... 33

Rocuronium bromide ............................ 59

Roflumilast............................................ 45

Romidepsin .......................................... 32

Roscovitine........................................... 27

Rosiglitazone........................................ 46

Rosiglitazone maleate .......................... 46

Rosuvastatin calcium ........................... 60

RVX-208............................................... 36

SS/GSK1349572 .................................... 49

Safinamide Mesylate ............................ 45

SAR131675 .......................................... 10

Saracatinib ........................................... 15

SB 202190............................................ 21

SB 216763............................................ 6

SB1317................................................. 20

SB203580............................................. 21

SB-269970 hydrochloride..................... 38

SB431542............................................. 13

SB-525334 ........................................... 30

SB590885............................................. 22

Natamycin ............................................ 54

Naxagolide ........................................... 52

Naxagolide Hydrochloride .................... 52

Necrostatin-1 ........................................ 18

Nelarabine ............................................ 53

Nepafenac ............................................ 38

Nepicastat hydrochloride...................... 52

Neratinib ............................................... 11

Niclosamide.......................................... 20

Nilotinib................................................. 16

Niltubacin.............................................. 31

NPI-2358 .............................................. 52

NSC 66811........................................... 18

NSC 74859........................................... 20

NU7026 ................................................ 35

NU7441 ................................................ 2

Nutlin-3 ................................................. 18

NVP-BEP800........................................ 23

NVP-BHG712 ....................................... 10

NVP-BSK805 dihydrochloride .............. 19

NVP-HSP990 ....................................... 23

NVP-TAE226........................................ 16

NXY-059............................................... 52

OOC000459 ............................................ 42

Odanacatib ........................................... 54

Oligomycin A ........................................ 43

Omecamtiv mecarbil............................. 54

Omeprazol ............................................ 49

Ondansetron hydrochloride .................. 38

ONX-0914 ............................................ 47

Oprozomib............................................ 47

Org 27569 ............................................ 40

Oseltamivir ........................................... 54

OSI-027 ................................................ 5

OSI-906 ................................................ 14

OSI-930 ................................................ 8

Ostarine................................................ 42

OSU-03012 .......................................... 6

Oxaliplatin............................................. 34

Oxcarbazepine ..................................... 59

PP22077 ................................................. 46

P505-15 hydrochloride ......................... 16

P5091 ................................................... 46

PA-824 ................................................. 56

PAC-1................................................... 18

Paclitaxel .............................................. 24

Palomid 529 ......................................... 5

Palonosetron hydrochloride.................. 38

Pamidronate disodium.......................... 58

Pazopanib ............................................ 8

PCI-24781 ............................................ 32

PCI-32765 ............................................ 16

PCI-34051 ............................................ 32

PD 0332991 ......................................... 27

PD 123319 ditrifluoroacetate................ 49

PD-0325901 ......................................... 19

PD173074 ............................................ 11

PD318088 ............................................ 19

PD98059 .............................................. 19

Pelitinib ................................................. 11

Pemetrexed disodium........................... 54

Perifosine ............................................. 4

PF-04217903........................................ 12

PF-04691502........................................ 3

PF-04929113........................................ 24

PF-2341066.......................................... 12

PF-4708671.......................................... 7

PF-477736............................................ 27

PF-4800567.......................................... 52

PF-562271............................................ 16

PH-797804 ........................................... 21

PHA-665752......................................... 13

PHA-739358......................................... 26

PHA-767491......................................... 28

PHT-427 ............................................... 4

PI-103................................................... 1

Piclamilast ............................................ 45

Pifithrin-α .............................................. 17

PIK-75 Hydrochloride ........................... 1

PIK-90 .................................................. 2

Pimecrolimus........................................ 57

Pirarubicin ............................................ 50

Pirfenidone ........................................... 30

Pizotifen malate.................................... 59

PJ34 hydrochloride............................... 33

PKI-179 ................................................ 1

PKI-587 ................................................ 1

Plerixafor .............................................. 40

PLX4032............................................... 22

PLX-4720 ............................................. 22

Pomalidomide....................................... 17

Posaconazole....................................... 56

PP121................................................... 9

PP2....................................................... 16

PP242................................................... 5

PQ401 .................................................. 14

Prasugrel .............................................. 40

Prasugrel hydrochloride ....................... 52

Praziquantel ......................................... 56

WY 14643............................................. 46

WYE-354 .............................................. 5

WYE-687 .............................................. 5

WZ 811................................................. 40

WZ4002................................................ 11

WZ8040................................................ 11

XX-376.................................................... 13

XAV939 ................................................ 25

XL147 ................................................... 2

XL-184.................................................. 12

XL228 ................................................... 14

XL388 ................................................... 5

XL765 ................................................... 2

XL888 ................................................... 24

YY-27632 dihydrochloride ...................... 29

ZZanamivir.............................................. 54

Zibotentan ............................................ 41

Zileuton................................................. 60

ZLN005................................................. 60

ZM 336372 ........................................... 22

ZM447439 ............................................ 26

ZSTK474 .............................................. 2

TG101209 ............................................ 19

TG101348 ............................................ 19

TGX-221............................................... 2

TH-302 ................................................. 44

Thalidomide.......................................... 17

Thiazovivin ........................................... 29

Tideglusib ............................................. 6

Tie2 kinase inhibitor ............................. 55

Tigecycline ........................................... 59

Tipifarnib............................................... 46

Tofacitinib ............................................. 19

Topotecan hydrochloride...................... 35

Torcetrapib ........................................... 44

Torin 1 .................................................. 5

Torin 2 .................................................. 5

Tosedostat............................................ 60

Tozasertib............................................. 26

TPCA-1................................................. 37

Trichostatin A ....................................... 31

Triciribine.............................................. 4

TSR-011 ............................................... 14

TSU-68 ................................................. 10

Tubacin................................................. 31

Tubastatin A hydrochloride................... 31

TW-37................................................... 17

TWS119 ............................................... 6

UU0126................................................... 19

Ubenimex ............................................. 47

UK 383367 ........................................... 57

VValproic acid sodium salt...................... 32

Vandetanib ........................................... 9

Vatalanib dihydrochloride ..................... 9

VE-821 ................................................. 34

Vicriviroc Malate ................................... 48

Vincristine sulfate ................................. 24

Vorinostat ............................................. 32

Vortioxetine hydrobromide ................... 38

VX-702 ................................................. 21

VX-770 ................................................. 43

VX-809 ................................................. 43

WWAY-362450 ........................................ 50

WAY-600 .............................................. 5

Wortmannin .......................................... 3

WP1066................................................ 19

WP1130................................................ 19

SB-705498 ........................................... 51

SB-743921 ........................................... 25

SB939................................................... 31

SC-514 ................................................. 37

SCH 900776......................................... 28

SCH527123.......................................... 40

SCH727965.......................................... 27

SCH772984.......................................... 19

Semagacestat ...................................... 46

SGI-1776 .............................................. 20

SGI-7079 .............................................. 12

SGX523................................................ 12

Sildenafil citrate .................................... 45

Sitagliptin phosphate monohydrate ...... 46

Sitaxsentan sodium .............................. 41

SKF 89976A hydrochloride .................. 39

SNS-032............................................... 28

Sorafenib Tosylate ............................... 8

Sotrastaurin .......................................... 30

SP600125............................................. 23

SRT1720 .............................................. 36

Staurosporine ....................................... 30

Stavudine ............................................. 49

Streptozotocin ...................................... 55

SU11274 .............................................. 12

SU5402 ................................................ 10

SU5416 ................................................ 9

Sulfadimethoxine.................................. 53

Sulfasalazine ........................................ 37

Sumatriptan succinate.......................... 38

Sunitinib Malate.................................... 8

Suvorexant ........................................... 41

SVT-40776 ........................................... 56

SYN115 ................................................ 52

TT0901317 ............................................. 50

TAK-438 ............................................... 43

TAK-632 ............................................... 22

TAK-733 ............................................... 18

TAK-875 ............................................... 42

TAK-901 ............................................... 27

Tamoxifen Citrate ................................. 60

Tamsulosin hydrochloride .................... 40

Tandutinib............................................. 15

Tariquidar ............................................. 43

Teicoplanin ........................................... 54

Telaprevir ............................................. 47

Telatinib ................................................ 9

Temozolomide...................................... 49

Tenovin-1 ............................................. 17

TG100-115 ........................................... 2

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