| 应用 |
A potent, reversible, and ATP-competitive inhibitor of Cdc7 and Cdk9 |
| 产品介绍 |
PHA-767491 (CAY10572)是ATP竞争性Cdc7和Cdk9抑制剂，IC50分别为10 nM和34 nM。 |
| 备注 |
PHA-767491 is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.It displays ~20-fold selectivity against CDK1/2 and GSK3-β, 50-fold selectivity against MK2 and CDK5, 100-fold selectivity against PLK |
| 生化机理 |
PHA-767491 (CAY10572) is a potent, ATP-competitive dual Cdc7/Cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication. Cdc7 kinase is known to promote the activity of DNA replication origins in eukaryotic organisms. Inhibition of Cdc7 kinase causes blockade of DNA synthesis in human cell lines. Tumor cells are then funneled into the apoptotic pathway in a p53-independent manner. Pharmacological inhibition of Cdc7 kinase can be an effective strategy for the development of oncologic therapeutics useful for treatment of cancers. At 10 μM, PHA-767491 induces apoptotic cell death in multiple cancer cell types. PHA-767491 also inhibits Cdk9, a kinase involved in the phosphorylation of RNA polymerase II and in transcriptional regulation of gene expression. |
| 别名 |
CAY10572;PHA767491;PHA 767491;1,5,6,7-四氢-2-(4-吡啶基)-4H-吡咯并[3,2-c]吡啶-4-酮;Cdc7/Cdk9 Inhibitor; CAY-10572;CAY 10572;PHA 767491; 2-Pyridin-4-yl-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one; 1,5,6,7-Tetrahydro-2-(4-pyridinyl)-4H-pyrrolo[3,2-c]pyridin-4-one |
