Description
Purvalanol A (212844-53-6) is a cyclin-dependent kinase inhibitor. IC50s= 4, 70, 35, 75 and 850 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk5/p35 and cdk4/cyclin D1 and respectively.1Reversibly arrests synchronized cells in G1 and G2 phase.2Induces ER stress-mediated apoptosis and autophagy in colon cancer cells.3Suppresses Src-mediated transformation by inhibiting both CDKs and c-Src.4In cells transformed with MYC, purvalanol A rapidly down-regulates survivin expression and induces MYC-dependent apoptosis.5Cell permeable.
Biological Activity
Cyclin-dependent kinase inhibitor. IC 50 values are 4, 70, 35, 850 and 75 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively. Reversibly arrests synchronised cells in G1 and G2, and inhibits cell proliferation and cell death.
References
[1] SERA T. [Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors].[J]. Tanpakushitsu kakusan koso. Protein, nucleic acid, enzyme, 2007, 52 13 Suppl: 1812-1813.
[2] NATHALIE VILLERBU. Cellular effects of purvalanol A: A specific inhibitor of cyclin-dependent kinase activities[J]. International Journal of Cancer, 2001, 97 6: 761-769. DOI:
10.1002/ijc.10125[3] AJDA COKER-GÜRKAN. Purvalanol induces endoplasmic reticulum stress-mediated apoptosis and autophagy in a time-dependent manner in HCT116 colon cancer cells.[J]. Oncology reports, 2015: 2761-2770. DOI:
10.3892/or.2015.3918[4] TOMOYA HIKITA Masato O Chitose Oneyama. Purvalanol A, a CDK inhibitor, effectively suppresses Src-mediated transformation by inhibiting both CDKs and c-Src.[J]. Genes to Cells, 2010, 15 10: 1051-1062. DOI:
10.1111/j.1365-2443.2010.01439.x[5] ANDREI GOGA. Inhibition of CDK1 as a potential therapy for tumors over-expressing MYC[J]. Nature Medicine, 2007, 13 7: 820-827. DOI:
10.1038/nm1606
