Purvalanol B

Biological Activity

Purvalanol B is a cyclin-dependent kinase (cdk) inhibitor (reported IC₅₀ values are 6 nM for cdk1 and cdk5, and 6 - 9 nM for cdk2, depending on binding partner). Purvalanol B is selective over a range of other protein kinases (IC₅₀ >10,000 nM). Purvalanol B shows antiproliferative properties, mediated by ERK1 and ERK2. Purvalanol B induces autophagy in cellular models and induces apoptosis in cancer cells, the apoptotic effects can be increased by combining with Rapamycin (Cat. No. 1292).

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Background References

1. How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
   Jorda et al.
   J.Med.Chem., 2018;61:9105
2. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.
   Gray et al.
   Science, 1998;281:533
3. ATP-site directed inhibitors of cyclin-dependent kinases.
   Gray et al.
   Curr.Med.Chem., 1999;6:859
4. p42/p44 MAPKs are intracellular targets of the CDK inhibitor purvalanol.
   Knockaert et al.
   Oncogene, 2002;21:6413

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