Purvalanol B

Purvalanol B (NG 95) 是选择性可逆的 ATP 竞争性 CDK 抑制剂。它在一系列其他蛋白激酶 (IC50>1000 nM) 中显示出对 CDK 的选择性。它抑制耐氯喹菌株 P. falciparum 的生长。

(S)-Purvalanol B 是 Purvalanol B 的 S 对映体，Purvalanol B 是一种细胞周期蛋白依赖性激酶（CDK）抑制剂。

Purvalanol A (NG-60) 是一种CDK 抑制剂，对 cdc2-cyclin B、cdc2-cyclin B、cdk2-cyclin E、cdk4-cyclin D1 和 cdk5-p35 的IC50值分别为 4、70、35、850 和 75 nM。

VMY-1-101 is a synthesized fluorescent CDK inhibitor. VMY-1-101 demonstrates potent CDK inhibitory activity, enhanced induction of G2 M arrest and modest apoptosis as compared to purvalanol B.

VMY-1-103 is a potent CDK inhibitor, is also a novel dansylated analog of purvalanol B, was shown to inhibit cell cycle progression and proliferation in prostate and breast cancer cells more effectively than purvalanol B. VMY-1-103 , but not purvalanol B, significantly decreased the proportion of cells in S phase and increased the proportion of cells in G(2) M. VMY-1-103 increased the sub G(1) fraction of apoptotic cells, induced PARP and caspase-3 cleavage and increased the levels of the Death Receptors DR4 and DR5, Bax and Bad while decreasing the number of viable cells, all supporting apoptosis as a mechanism of cell death. VMY-1-103 possesses unique antiproliferative capabilities and that this compound may form the basis of a new candidate drug to treat medulloblastoma.