MK-1775(AZD-1775,Adavosertib)
CAS 955365-80-7
Adavosertib (AZD-1775; MK-1775) is a potent Wee1 inhibitor with an IC50 of 5.2 nM.
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MK-8776 (SCH 900776)
CAS 891494-63-6
SCH900776 is a potent, selective and oral inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. It shows 50- and 500-fold selectivity over CDK2 andChk2, respectively.
NSC-664704(Kenpaullone)
CAS 142273-20-9
Kenpaullone is an ATP-competitive inhibitor of several cyclin-dependent kinases (CDKs) as well as glycogen synthase kinase 3β (GSK3β).It inhibits GSK3β with an IC50 value of 0.023 µM (0.23 µM) and Cdk1/cyclin B, Cdk2/cyclin A, Cdk5/p25, and lymphocyte kinase…
Docetaxel
CAS 114977-28-5
Docetaxel is an antineoplastic drug by inhibiting microtubule depolymerization, and attenuating of the effects of bcl-2 and bcl-xL gene expression.
VE-821
CAS 1232410-49-9
VE-821 is a potent ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM.
Fludarabine phosphate
CAS 75607-67-9
Fludarabine (phosphate) is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.
SCH900776 S-isomer
CAS 891494-64-7
SCH900776 S-isomer is the S-isomer of SCH900776. SCH900776 is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with IC50 of 3 nM.
RGB286638
CAS 784210-88-4
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with…
Paclitaxel
CAS 33069-62-4
Paclitaxel is a potent anticancer medication which can promote microtubule (MT) assembly, inhibit MT depolymerization, and change MT dynamics required for mitosis and cell proliferation.
PHA-793887
CAS 718630-59-2
PHA-793887 is a potent, ATP-competitive CDK inhibitor, can inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC50s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with an IC50 of 79 nM.
THZ1 free base
CAS 1604810-83-4
THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM.
LY2334737
CAS 892128-60-8
LY2334737 is an orally available prodrug of gemcitabine which is a nucleoside analog used as chemotherapy.IC50 Value:Target: Nucleoside analogin vitro: Five cell lines that express CES2 responded to LY2334737treatment. LY2334737 was less cytotoxic to a…
AZ-6102
CAS 1645286-75-4
AZ6102 is a potent dual TNKS1 and TNKS2 inhibitor, with IC50s of 3 nM and 1 nM, respectively, and alao has 100-fold selectivity against other PARP family enzymes, with IC50s of 2.0 μM, 0.5 μM, and >3 μM, for PARP1, PARP2, and PARP6, respectively.
MK-5108
CAS 1010085-13-8
MK-5108 inhibits Aurora-A activity in an ATP-competitive manner. MK-5108 shows robust selectivity against the other family kinases Aurora-B (220-fold) and Aurora-C (190-fold) in the biochemical assay. MK-5108 also reveals high selectivity For Aurora-A over…
CCT244747
CAS 1404095-34-6
CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.
beta-Lapachone (ARQ-501, CO-501)
CAS 4707-32-8
Beta-Lapachone inhibits DNA relaxation induced by DNA topoisomerase I in a dose-dependent manner. Treatment of beta-lapachone (100 nM or greater) results in >95% inhibition of Topo I DNA unwinding activity compared to the DMSO control. beta-lapachone (1-5 μM)…
ON123300
CAS 1357470-29-1
ON123300 is a potent inhibitor of CDK4, with an IC50 of 3.8 nM, with little inhibitory activity against CDKs 1,2,5 and 8.
Carmustine
CAS 154-93-8
Carmustine is an antitumor chemotherapeutic agent, which works by akylating DNA and RNA.
Nutlin-3a
CAS 675576-98-4
Nutlin 3a is an active enantiomer of Nutlin-3, acts as a murine double minute (MDM2) antagonist that inhibits MDM2-p53 interactions and stabilizes the p53 protein, and thereby induces cell cycle arrest and apoptosis.
MLN8237 (Alisertib)
CAS 1028486-01-2
Alisertib (MLN 8237) is a selective Aurora A inhibitor with an IC50 of 1.2 nM.
Niraparib tosylate
CAS 1038915-73-9
Niraparib tosylate (MK-4827 tosylate) is an excellent PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively.
CVT-313(NG-26)
CAS 199986-75-9
CVT-313 is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM.
AZ20
CAS 1233339-22-4
AZ20 is a potent and selective inhibitor of ATR with an IC50 of 5 nM, and has 8-fold selectivity against mTOR (IC50=38 nM).
ENMD-2076
CAS 934353-76-1
ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
NVP-TNKS656
CAS 1419949-20-4
NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM, and is > 300 fold selectivity against PARP1 and PARP2.
E-7449
CAS 1140964-99-3
E7449 is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ∼50 and ∼50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate.
Compound 401
CAS 168425-64-7
Compound 401 is a synthetic inhibitor of DNA-PK (IC50 = 0.28 μM) that also targets mTOR but not PI3K in vitro.
MPI-0479605
CAS 1246529-32-7
MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC50 of 1.8 nM.
Evofosfamide(TH-302)
CAS 918633-87-1
Evofosfamide (TH-302) is a hypoxia-activated prodrug with IC50 of 10 μM and 1000 μM in hypoxia (N2) and normoxia (21% O2), respectively.
Irinotecan
CAS 97682-44-5
Irinotecan is a water soluble topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.
Mad2 inhibitor-1 (M2I-1)
CAS 312271-03-7
M2I-1 a small Mad2 inhibitor-1. the first small molecule inhibitor targeting the binding of Mad2 to Cdc20, an essential proteinprotein interaction (PPI) within the SAC. It can disturbs conformational dynamics of Mad2 critical for complex formation with Cdc20.…
Eg5 Inhibitor III（Dimethylenastron）
CAS 863774-58-7
Dimethylenastron is a potent Eg5 inhibitor, with an IC50 of 200 nM.
GJ103 (sodium salt)
CAS 1459687-96-7
GJ103 sodium salt is an active analog of the read-through compound GJ072.
SU5614
CAS 1055412-47-9
(Z)-SU5614 is a potent FLT3 inhibitor and selectively induces growth arrest, apoptosis, and cell cycle arrest in Ba/F3 and AML cell lines expressing a constitutively activated FLT3[1].
ABT-751(E 7010)
CAS 141430-65-1
ABT-751(E 7010) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and 3.4 μM in neuroblastoma and non-neuroblastoma cell lines, respectively.
Madrasin
CAS 374913-63-0
Madrasin is a potent and cell penetrant splicing inhibitor that interferes with the early stages of spliceosome assembly. Madrasin is cytotoxic at higher concentrations, although at lower concentrations it induces cell cycle arrest, promotes a specific…
Nedaplatin (Aqupla)
CAS 95734-82-0
Nedaplatin is a derivative of cisplatin and DNA damage agent.Target: OthersNedaplatin(NDP) is a derivative of cisplatin which produced less nausea & vomiting and nephrotoxicity. the effect of NDP on the 7-ethyl-1-hydroxy-CPT (the active form of…
PHA-739358 (danusertib)
CAS 827318-97-8
Description of Danusertib: Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Aurora kinase inhibitor PHA-739358 binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in…
WHI-P180(Janex 3)
CAS 211555-08-7
WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively.
SW-044248
CAS 522650-83-5
SW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.
SN-38(NK-012)
CAS 86639-52-3
SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively.
Cyclovirobuxin D(Bebuxine)
CAS 860-79-7
Cyclovirobuxine D (CVB-D) is the main active component of the traditional Chinese medicine Buxus microphylla. Cyclovirobuxine D induces autophagy and attenuates the phosphorylation of Akt and mTOR[1]. Cyclovirobuxine D inhibits cell proliferation of gastric…
SB-715992 (Ispinesib)
CAS 336113-53-2
Ispinesib is a specific inhibitor of KSP, with a Ki app of 1.7 nM.
Arranon
CAS 121032-29-9
Nelarabine (Arranon, 506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells. Nelarabine is a chemotherapy drug used in T-cell acute lymphoblastic leukemia.
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