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You are here:Home-Inhibitors & Agonists-Cell Cycle/DNA Damage-Checkpoint Kinase (Chk)

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    Checkpoint Kinases (Chk) are protein kinases that are involved in cell cycle control. Two checkpoint kinase subtypes have been identified, Chk1 and Chk2. Chk1 is a central component of genome surveillance pathways and is a key regulator of the cell cycle and cell survival. Chk1 is required for the initiation of DNA damage checkpoints and has recently been shown to play a role in the normal (unperturbed) cell cycle. Chk1 impacts various stages of the cell cycle including the S phase, G2/M transition and M phase. In addition to mediating cell cycle checkpoints, Chk1 also contributes to DNA repair processes, gene transcription, embryo development, cellular responses to HIV infection and somatic cell viability.

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    Chk2 is a protein kinase that is activated in response to DNA damage and is involved in cell cycle arrest. In response to DNA damage and replication blocks, cell cycle progression is halted through the control of cell cycle regulators. The protein encoded by this gene is a cell cycle checkpoint regulator and putative tumor suppressor.

Cat. No. Product Name CAS No. Information
H1903

CHIR-124

 		405168-58-3

CHIR-124 is a potent, selective Chk1 inhibitor with in vitro IC50 of 0.3 nM, 2,000-fold selectivity over Chk2; displays 500- to 5,000-fold less active against other cell cycle kinases, such as CDK2/cyclin A , Cdc2/cyclin B, and CDK4/cyclin D; also potently inhibits PDGFR and FLT3 with IC50s of 6.6 nM and 5.8 nM; interacts synergistically with topoisomerase poisons (e.g., camptothecin or SN-38) in causing growth inhibition in several p53-mutant solid tumor cell lines, abrogates the SN-38-induced S and G2-M checkpoints and potentiates apoptosis in MDA-MD-435 breast cancer cells, also restores the level of cdc25A protein; potentiates the growth inhibitory effects of irinotecan in breast cancer xenograft models.
H1902

CCT241533 hydrochloride

 		1431697-96-9

A potent and selective ATP-competitive inhibitor of CHK2 K5777:N5777with IC50 of 3 nM; shows good selectivity for CHK2 against CHK1 (IC50=180 nM) and a wider panel of kinases and with promising in vitro ADMET properties; inhibits CHK2 autophosphorylation at S516, band shift mobility changes, and HDMX degradation.

H1901

CCT241533

 		1262849-73-9

A potent and selective ATP-competitive inhibitor of CHK2 K5777:N5777with IC50 of 3 nM; shows good selectivity for CHK2 against CHK1 (IC50=180 nM) and a wider panel of kinases and with promising in vitro ADMET properties; inhibits CHK2 autophosphorylation at S516, band shift mobility changes, and HDMX degradation.

H1900

CCT-245737

 		1489389-18-5

A highly potent, selective, ATP-competitive inhibitor of Chk1 with IC50 of 1.3 nM; weak inhibition on Chk2 (IC50=2440 nM); inhibits genotoxic-induced CHK1 activity (pS296 CHK1) and cell cycle arrest (pY15 CDK1) both in vitro and in human tumor xenografts; showes significant single-agent activity against a MYC-driven mouse model of B-cell lymphoma; orally active.
H1899

CCT-244747

 		1404095-34-6

A novel, potent, highly selective, orally active, ATP competitive CHK1 inhibitor with biochemical IC50 of 8 nM; displays 75-fold selectivity against FLT3 and >1,000-fold selectivity against CHK2 and CDK1; inhibits cellular CHK1 activity (IC50=29-170nM), significantly enhances the cytotoxicity of several anticancer drugs and abrogates drug-induced S and G2 arrest in multiple tumor cell lines; enhances antitumor activity of gemcitabine and irinotecan in vivo.
H1898

BAY-1816032

 		1891087-61-8

BAY-1816032 (BAY1816032) is a highly potent, selective, orally active BUB1 mitotic checkpoint serine/threonine kinase with IC50 of 7 nM, displays excellent selectivity on a panel of 395 kinases; abrogates nocodazole-induced Thr-120 phosphorylation of the major BUB1 target protein histone H2A in HeLa cells with IC50 of 29 nM, induces lagging chromosomes and mitotic delay, inhibits proliferation of various tumor cell lines with mean IC50 of 1.4 uM; demonstrates synergy or additivity with paclitaxel or docetaxel both in vitro and in vivo.
H1897

AZD-7762

 		860352-01-8

AZD-7762 (AZD7762) is a?potent and selective inhibitor of Chk1/2 with IC50 of 5 nM; shows less potent against CAM, Yes, Fyn, Lyn, Hck and Lck; enhances the radiosensitivity of mutated p53 tumor cell lines and HT29 xenografts.

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