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CDK inhibitor
BMS-265246 is a potent new pyra- zolopyridine inhibitor of cdk2/cyclin E and cdk1/cyclin B, as well as cdk4/cyclin D. -
Cdc7/cdk9 inhibitor
PHA-767491 is a potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication.
- Lei Tan, .et al. , Res Vet Sci, 2022, 145: 125-134 PMID: 35190327
- Qi Li, .et al. , Transl Oncol, 2018, Apr; 11(2): 300-306 PMID: 29413763
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Chk1 inhibitor
SCH900776 is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities. It specifically binds to and inhibits Chk1, which may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases to undergo DNA repair prior to entry into mitosis; tumor cells may thus be sensitized to the DNA-damaging effects of ionizing radiation and alkylating chemotherapeutic agents.
- Hong Yang, .et al. , Research Square, 2022, May 9th
- Motofumi Suzuki, .et al. , Int J Radiat Oncol Biol Phys, 2021, May 25;S0360-3016(21)00361-8 PMID: 34112559
- Min Wu, .et al. , Haematologica, 2019, 104 PMID: 30975911
- Permata TBM, .et al. , Oncogene, 2019, Feb 12 PMID: 30755733
- Hiro Sato, .et al. , Nat Commun, 2017, 8: 1751 PMID: 29170499
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Aurora Kinase B/C inhibitor
GSK1070916 is a potent Aurora B/C kinase inhibitor (with IC50 of 3.5 nM/6.5 nM) with broad antitumor activity in tissue culture cells and human tumor xenograft models.
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Aurora A/B Kinase inhibitor
PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1. -
CDK inhibitor
Kenpaullone is a potent inhibitor of CDK1/cyclin B (IC?????€ = 400 nM), CDK2/cyclin A (IC?????€ = 680nM) , CDK5 (IC?????€ = 850nM) and with much less effect other kinases.- Katelyn M Green, .et al. , J Biol Chem, 2019, jbc.RA119.009951
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multi-kinase inhibitor
Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. -
CDK inhibitor
AT7519 is an inhibitor of multiple cyclin-dependent kinases (CDKs), which may result in cell cycle arrest, induction of apoptosis, and inhibition of tumor cell proliferation. -
Aurora A Kinase inhibitor
MK-5108, also known as VX-689, is a competitive inhibitor of the ATP-binding site of aurora A kinase.- Wei TW, .et al. , Cancer Res, 2017, Jan 15;77(2):494-508 PMID: 28069801
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PLK1/PLK3 inhibitor
GW843682X is a selective inhibitor of polo-like kinase 1 (PLK1) and polo-like kinase 3 (PLK3) (IC50 values are 2.2 and 9.1 nM respectively).- Kanada F, .et al. , Sci Rep, 2019, Dec 27;9(1):20085 PMID: 31882756
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ROCK inhibitor
Y-33075 dihydrochloride is a selective ROCK inhibitor with an IC50 of 3.6 nM. -
FLT3 inhibitor
TG-02 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor. -
Ca2+ channel agonist/CDK2 inhibitor
Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction. -
ROCK inhibitor
GSK 269962 is a potent Rho kinase (ROCK) inhibitor (IC50 values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively).- Praneeth Siripurapu, .et al. , J Biol Chem, 2017, Oct 20; 292(42): 17482-17495 PMID: 28864771
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CDK inhibitor
Purvalanol B is a cyclin-dependent kinase inhibitor. IC50 values are 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively. Selective over a range of other protein kinases (IC50 > 10,000 nM). -
CDK8 inhibitor
MSC2530818 is a potent, selective and orally available CDK8 inhibitor with an IC50 of 2.6 nM for CDK8. -
ROCK inhibitor
SR 3677 dihydrochloride is a potent and selective Rho-kinase inhibitor (IC50 values are 3 and 56 nM for ROCK-II and ROCK-I respectively). -
CHK1 Inhibitor
SCH900776 is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities. - Pyridostatin is a G-quadruplex-interacting drug which can promote growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage.
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CDK inhibitor
BAY 1000394 is an orally bioavailable cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity.- Marzia Ognibene, .et al. , Sci Rep, 2020, 10: 12902 PMID: 32737364
- Xinan (Holly) Yang, .et al. , Sci Rep, 2017, 7: 41 PMID: 28246384
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Cdc42 GTPase inhibitor
CASIN is a novel and potent Cdc42 inhibitor.- Yongru Xu, .et al. , Int J Mol Sci, 2017, Mar; 18(3): 586 PMID: 28282856
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KRas G12C inhibitor
KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1. -
CDK4/6 inhibitor
LY2835219 is an orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity.- Elaheh S Abutorabi, .et al. , Mol Biol Rep, 2023, May;50(5):4073-4082 PMID: 36877344
- Yoshinori Tanaka, .et al. , Biochem Biophys Res Commun, 2022, Jul 23;614:191-97 PMID: 35598430
- Sumire Suzuki, .et al. , Oncol Rep, 2022, Feb;47(2):40 PMID: 34958115
- Kana Nakatani, .et al. , Int J Hematol, 2020, Oct 17 PMID: 33068248
- Ryohei Ogata, .et al. , Breast Cancer, 2020, Aug 28 PMID: 32860163
- Elaheh Seyed Abutorabi, .et al. , Rep Biochem Mol Biol, 2020, Jan; 8(4): 438-445 PMID: 32582803
- Hidemasa Matsuo, .et al. , Blood Adv, 2018, Nov 13; 2(21): 2879-2889 PMID: 30381403
- Iriyama N, .et al. , Leuk Lymphoma, 2018, Jun;59(6):1439-1450 PMID: 28918692
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Kras-G12C inhibitor
KRas G12C inhibitor 3 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.