货号：A421689同义名：
Cdk2 Inhibitor III; Cyclin-dependent kinase 2 Inhibitor III
CVT-313 is a potent, selective, ATP-competitive and reversible inhibitor of CDK2 with IC50 of 0.5 μM for Cdk2/A and Cdk2/E; 4.2 μM for Cdk1/B; 215 μM for Cdk4/D1.
Cell cycle progression in mammalian cells is regulated by a family of cyclin-dependent protein kinases (CDKs). CDK2 is a serine/threonine kinase whose activity is essential for the G1 to S transition during cell division. CVT-313 is a potent, selective and ATP-competitive CDK2 inhibitor with an IC50 of 0.5 μM and a Ki of 95 nM, and has no effect on other, nonrelated ATP-dependent serine/threonine kinases. The growth of mouse, rat, and human cells in culture was inhibited by CVT-313 with the IC50 for growth arrest ranging from 1.25 to 20 μM. When nonsynchronized MRC-5 cells were treated with CVT-313 (6.25 μM) for 36 h, most of these cells had a 2 N DNA content, consistent with a G1/S arrest. After removal of CVT313, cells reentered the cell cycle suggesting that the inhibition of cell proliferation was reversible. Moreover, if CVT-313 (6.25 mM) was added at 0, 4, or 8 h after serum stimulation, Rb hyperphosphorylation was inhibited. A brief intraluminal exposure of CVT-313 (1.25 mg/kg for 15 min) to a denuded rat carotid artery resulted in more than 80% inhibition of neointima formation[3].
搜索
