Drug intelligence / Profile preview

purvalanol a

Development stage
Preclinical
Modality
Small Molecules
Administration
In Vitro/research Use Only (not Approved For Human Administration)
01

Overview

Purvalanol A is a potent, cell-permeable, reversible small molecule inhibitor of cyclin-dependent kinases (CDKs), particularly CDK2. It also inhibits other kinases such as DYRK1A and has activity against c-Src tyrosine kinase. By inhibiting CDKs, Purvalanol A disrupts the formation and function of CDK-cyclin complexes necessary for cell cycle progression. This leads to cell cycle arrest at G1 and G2 phases and can trigger apoptosis in cancer cells through caspase-dependent mechanisms. The drug has been shown to upregulate polyamine catabolic enzymes (such as SSAT and PAO), contributing to its pro-apoptotic effects in certain cancer models. Additionally, it suppresses c-Src-mediated transformation by inhibiting both CDKs and c-Src activity[1][5][7]. Purvalanol A is used primarily as an experimental tool compound in research settings; it is not approved for clinical use.

Other names
2-(1R-Isopropyl-2-hydroxyethylamino)-6-(3-chloroanilino)-9-isopropylpurine(R)-2-((6-((3-Chlorophenyl)amino)-9-isopropyl-9H-purin-2-yl)amino)-3-methylbutan-1-ol212844-53-6
02

Targets

CDK2 (Cyclin-dependent kinase 2)CDK7DYRK1A (Dual-specificity tyrosine-phosphorylation-regulated kinase 1A)RPS6KA1 (Ribosomal S6 kinase Alpha-1)CDK1 (Cyclin-dependent kinase 1)CDK5 (Cyclin-dependent kinase 5)

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