Purvalanol A (NG-60) is an effective and cell-permeable CDK inhibitor with IC50 of 70/4/35/850 nM for cdk2-cyclin A/B/E, and cdk4-cyclin D1, respectively.

CDK4-CyclinD1:850 nM, CDK2-CyclinE:35 nM, CDC2-cyclinB:4 nM, CDK2-CyclinA:70 nM

在MCF-7细胞中,Purvalanol A使细胞活性损失50%,但MDA-MB-231细胞对Purvalanol A的敏感性相对较低(细胞活性减少32 %)。在MCF-7和MDA-MB-231细胞中,Purvalanol A可促使线粒体介导的细胞凋亡。Purvalanol A可使MCF-7和MDA-MB-231细胞系的细胞活性降低,该作用具有剂量依赖性。通过抑制细胞周期进程和c-Src信号通路,Purvalanol A可有效防止c-Src介导转化,且对一些c-Src上调的人类癌细胞贴壁不依赖性生长有明显的抑制效果。Purvalanol A可显著抑制HT29和SW480人结肠癌细胞的贴壁依赖性生长。

Cells are seeded at 10000 density in 96-well plates and treated with various concentrations of Purvalanol A (0-100 μM) for 24 h. Cells are exposed to 10 μL of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltet- razolium bromide dye (5 mg/mL) and are incubated at 37℃ for 4 h. In order to solubilize the formazan crystals 100 μL DMSO is added. Absorbance is determined at 570 nm spectrophotometrically.(Only for Reference)