Purvalanol B

基本信息

产品描述

Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitor with IC50 values of 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively. IC50 Value: 6 nM(cdc2/cyclin B); 6 nM(cdk2/cyclin A); 9 nM(cdk2/cyclin E); 6 nM(cdk5-p35)[1] Target: cdc2/cyclin B; cdk2/cyclin E; cdk5-p35 in vitro: In vitro inhibitory activity against Cyclin-dependent kinase 1-cyclin B complex from starfish oocytes is 6 nM (IC50) [1]. In addition to CDK1, p42/p44 MAPK were found to be two major purvalanol-interacting proteins in five different mammalian cell lines (CCL39, PC12, HBL100, MCF-7 and Jurkat cells), suggesting the generality of the purvalanol/p42/p44 MAPK interaction. When cells were treated with purvalanol, p42/p44 MAPK and CDK1 activities were inhibited in a dose-dependent manner. Furthermore, purvalanol inhibited the nuclear accumulation of p42/p44 MAPK, an event dependent on the catalytic activity of these kinases [2]. in vivo:

靶点（IC50 & Targe）

Cdk2/cyclin A,6 nM

Cdk2/cyclin E,9 nM

Cdk5/p35,6 nM

Cdk2/cyclin B,6 nM

参考文献

[1]. purvalanol B (CID 448991) - Compound BioActivity Data

[2]. Knockaert M, et al. p42/p44 MAPKs are intracellular targets of the CDK inhibitor purvalanol. Oncogene. 2002 Sep 19;21(42):6413-24.