产品描述:
Aminopurvalanol A is a selective, cell-permeable, and competitive cyclin-dependent kinase (CDK) inhibitor that potently inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p35 (IC50s = 33, 33, 28, and 20 nM, respectively).{39089} It is over 90-fold selective for CDKs over ERK1, ERK2, PKC-δ, protein kinase A (PKA), casein kinase 1, insulin receptor tyrosine kinase (IC50s = 3.0-36 μM), and over 3,000-fold selective over a range of other kinases (IC50s > 100 μM). In antiproliferative assays in vitro, aminopurvalanol A inhibits growth of ovarian (IGROV1), leukemic (SR), lung (NCI-H522), and colonic (KM12) cells (GI50s = 470, 420, 1,000, and 30 nM, respectively). Aminopurvalanol A also inhibits mitotic division and preferentially arrests cells in the G2/M phase via Cdk1/cyclin B{39090,39091}