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Aurora inhibitor
PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3. -
CDK Inhibitor
PHA-793887, a novel potent inhibitor of Cdk, target on kinds of cyclin-dependent kinase under low concentrations and poses high activity against several cancer cell lines.- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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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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FLT3 inhibitor
TG-02 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor. -
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). -
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. -
IGF-1R, Aurora, FGFR, ABL, SRC inhibitor
XL228 is a protein kinase inhibitor targeting IGF1R, the AURORA kinases, FGFR1-3, ABL and SRC family kinases. XL228 is an Aurora A inhibitor (IC50, f3 nmol/L) that has shown potent biochemical activity against ABL1 (Ki, 5 nmol/L), as well as the BCR-ABL1 T315I (Ki, 1.4 nmol/L) kinases. -
Cdc25 inhibitor
NSC 663284 is a potent, cell-permeable, and irreversible inhibitor of all Cdc25 isoforms, with preference for Cdc25A (IC50 = 29, 95, and 89 nM for Cdc25A, Cdc25B2, and Cdc25C, respectively). -
CDK4/6 inhibitor
LEE011 is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity.- Federico Antoniciello, .et al. , Front Mol Biosci, 2023, May 11;9:887564 PMID: 35647033
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Chk1 inhibitor
LY2606368 is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.- Yuri Tozaki, .et al. , Cancers (Basel), 2023, Jan 25;15(3):735 PMID: 36765693
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PLK inhibitor
SBE 13 HCl is a selective inhibitor of PLK1 (IC50 values are 200 pM, 875 nM and 66 μM for PLK1, PLK3 and PLK2 respectively). -
CDK inhibitor
AT7519 trifluoroacetate is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM, less potent to CDK3 and little active to CDK7. -
ROCK activator
Narciclasine is a Rho/Rho kinase/LIM kinase/cofilin signaling pathway activator. -
ROCK inhibitor
SAR407899 is a potent and selective Rho kinase inhibitor with promising antihypertensive activity. -
CDC7 inhibitor
LY-3177833 is a potent and selective inhibitor of CDC7 (Cell Division Cycle 7-related Protein Kinase). -
CDK inhibitor
Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively. -
KRAS G12C covalent inhibitor
AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity. -
Aurora A kinase inhibitor
Aurora Kinase Inhibitor 3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50>10 μM. -
G-quadruplexe stabilizer
Pyridostatin hydrochloride (RR82 hydrochloride) is a G-quadruplexe stabilizer, with a Kd of 490 nM.
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