Drug intelligence / Profile preview

aminopurvalanol a

Development stage
Discontinued
Lead developer
University of California
Modality
Small Molecules
Administration
In Vitro (research Use Only)
01

Overview

Aminopurvalanol A is a potent, selective, and cell-permeable small molecule inhibitor of cyclin-dependent kinases (CDKs), specifically targeting CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, and CDK5/p35 complexes with low nanomolar IC50 values. It acts as an ATP-competitive inhibitor by binding to the ATP-binding pocket of these kinases. Aminopurvalanol A also inhibits ERK1 and ERK2 at higher micromolar concentrations but is highly selective over other protein kinases. Its primary biological effects include arresting the cell cycle at the G2/M boundary and inducing apoptosis at higher concentrations. The compound displays anti-mitotic and anti-tumor properties in vitro and is primarily used as a research tool for studying cell cycle regulation, cancer progression mechanisms, kinase signaling pathways, and reproductive biology[1][3][4][5][7][9].

Other names
(2R)-2-((6-((3-amino-5-chlorophenyl)amino)-9-(1-methylethyl)-9H-purin-2-yl)amino)-3-methyl-1-butanolNG-97NG97NG 97
02

Targets

CDK1 (Cyclin-dependent kinase 1)MAPK3 (Mitogen-activated protein kinase 1)CDK5 (Cyclin-dependent kinase 5)CDK2 (Cyclin-dependent kinase 2)

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