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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.
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 |
---|---|---|---|
GY03968 |
SB218078 |
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. |
GY02620 |
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. |
GY02560 |
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. |
GY02503 |
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. |
GY07052 |
MU 380 |
2109805-78-7 | MU 380 is a novel potent, selective CHK1 inhibitor 2 nM, >80-fold selectivity over CHK2; sensitizes a variety of tumor cell lines to hydroxyurea or gemcitabine up to 10 times; shows extended inhibitory effects in cells, and unlike SCH900776, does not undergo in vivo N-dealkylation to the significantly less selective metabolite; causes higher accumulation of DNA damage in tumor cells and subsequent enhanced cell death, and is more efficacious in the A2780 xenograft mouse model. |
GY06980 |
Debromohymenialdisine |
75593-17-8 | Debromohymenialdisine is a marine sponge alkaloid that inhibits Chk1 and Chk2 with IC50 of 3 and 3.5 uM, respectively; also inhibits MAP kinase kinase 1 (IC50=881 nM), GSK3β (IC50=1.39 uM), and CDK5/p25 (IC50=9.12 uM), does not significantly affect ATM and ATR; blocks G2 arrest in cancer cells. |
GY06979 |
PD-321852 |
622856-21-7 | PD-321852 is a potent, reasonably selective Chk1 inhibitor with cell IC50 of 5 nM; potentiates gemcitabine-induced clonogenic death in a panel of pancreatic cancer cell lines; inhibits gemcitabine-induced Rad51 focus formation, and depletes RAD51 proteins in pancreatic cancer cells. |
GY05347 |
GDC-0575 |
1196541-47-5 | GDC-0575 (ARRY-575, RG-7741) is a potent, selective and orally bioavailable Chk1 inhibitor with IC50 of 1.2 nM; enhances the killing of primary AML cells ex vivo by inducing apoptosis combined with AraC, blocks the activation of CHK1 induced by AraC via decrease in the level of Tyr15-phosphorylated CDK2 at 100 nM in AML cells. |
GY02328 |
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. |
GY02281 |
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. |
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