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Purvalanol A

CAS No. : 212844-53-6

MCE 国际站：Purvalanol A

产品活性：Purvalanol A 是一种有效的 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。

研究领域：Cell Cycle/DNA Damage  |  Autophagy  |  Apoptosis

作用靶点：CDK  |  Autophagy  |  Apoptosis

In Vitro: Purvalanol A inhibits cdc28 (S. cerevisiae) and erk1 with IC₅₀s of 80 and 9000 nM. Purvalanol A shows inhibitory activities against the NCI panel of 60 human tumor cell lines, with average GI50 of 2 μM; two cell lines show an -20-fold increase in sensitivity to purvalanol A: the KM12 colon cancer cell line with a GI₅₀ of 76 nM and the NCI-H522 non–small cell lung cancer cell line with a GI₅₀ of 347 nM. Purvalanol A is a 2.5-fold more potent inhibitor of CDK2, but also inhibits DYRK1A potently and a number of other protein kinases in the low micromolar range. Purvalanol A inhibits MKK1, MAPK2/ERK2, JNK/SAPK1c with IC₅₀s of 80, 26, 84 μM. Purvalanol A selectively inhibits the phosphorylation of cellular proteins. Purvalanol A prevents the increases of the contents of cyclins D and E during serum-induced G1 phase progression. Purvalanol A does not inhibit transcription under cell-free conditions.

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