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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
H1925	XL-844	631864-00-1	A potent, specific, orally available, ATP‑competitive inhibitor of Chk1 and Chk2 with Ki of 2.2 nM and 0.07 nM, respectively; increases gemcitabine-induced H2AX phosphorylation, blocks Cdc25A phosphorylation, and induces premature mitotic entry; significantly enhances gemcitabine antitumor activity in a PANC-1 xenograft model.
H1924	VRX-0466617	926906-64-1	A potent and selective Chk2 inhibitor with Ki/IC50 of 11 nM/120 nM; shows no inhibitory effect on Chk1 (>100 uM); inhibits the phosphorylation of Chk2 Ser(19) and Ser(33-35), but not of Chk2 Thr(68), prevents the IR-induced Chk2-dependent degradation of Hdmx and attenuates IR-induced apoptosis.
H1922	VER-158411	1174664-88-0	A potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively; dispalys >1,000-fold selectivity over CDK1; reduces pChk1 (S296) and pChk2 (S516) levels in a concentration dependent fashion in cells treated with etoposide with IC50s of 48 nM for Chk1 and 904 nM for Chk2; potentiates the cytotoxicity of chemotherapeutic agents in a variety of p53 deficient human tumor cell lines (GI50=0.5-9.5 uM) and human colon tumor xenograft models.
H1921	SB-218078	135897-06-2	A potent inhibitor of Chk1 that blocks phosphorylation of cdc25 with IC50 of 15 nM; less potently inhibits Cdc2 and PKC (IC50=250 and 1,000 nM, respectively) and causes 85% inhibition of PKD1 at 1 uM; enhances the cytotoxicity of DNA-damaging agents.
H1919	SAR-020106	184843-57-9	SAR-020106 is a potent, selective, ATP-competitive Chk1 inhibitor with IC50 of 13.3 nM; brogates the etoposide-induced G(2) arrest with IC50 of 55 nM in HT29 cells, significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro; inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 both in vitro and in vivo; enhances irinotecan and gemcitabine antitumor activity in mice with minimal toxicity.
H1918	PV-1115	1093793-10-2	A potent and highly selective Chk2 inhibitor with IC50 of 0.14 nM; displays greater than 100 uM for Chk1 in vitro.
H1917	PV-1019		A potent, ATP-competitive and highly selective Chk2 inhibitor with IC50 of 138 nM; displays much reduced or no activity against a panel of 52 other cellular kinases, including Chk1; inhibits Chk2-mediated phosphorylation of Cdc25C (IC50=260 nM), and nd HDMX degradation in response to DNA damage; protects normal mouse thymocytes against ionizing radiation-induced apoptosis.
H1916	Prexasertib dihydrochloride	1234015-54-3	A potent, selective, ATP-competitive inhibitor of CHK1 with Ki of 0.9 nM; potently abrogates the G2-M checkpoint activated by doxorubicin in p53-deficient HeLa cells with EC50 of 9 nM; causes replication catastrophe in vitro and in vivo; shows significant tumor growth inhibition in xenograft tumor models.
H1915	Prexasertib	1234015-52-1	A potent, selective, ATP-competitive inhibitor of CHK1 with Ki of 0.9 nM; potently abrogates the G2-M checkpoint activated by doxorubicin in p53-deficient HeLa cells with EC50 of 9 nM; causes replication catastrophe in vitro and in vivo; shows significant tumor growth inhibition in xenograft tumor models.
H1914	PF-00477736	952021-60-2	PF-00477736 (PF-477736) is a potent, selective, ATP-competitive inhibitor of Chk1 with Ki of 0.49 nM, also inhibits Chk2 (Ki=47 nM) and poorly inhibits CDK1 activity (Ki=9.9 uM); displays 100 protein kinases; abrogates cell cycle arrest induced by DNA damage and enhances cytotoxicity of clinically important chemotherapeutic agents, including gemcitabine and carboplatin; enhances the antitumor activity of gemcitabine in a dose-dependent manner in xenografts.

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