(2R)-2-[[6-[(3-CHLORO-4-CARBOXYPHENYL)AMINO]-9-(1-METHYLETHYL)-9H-PURIN-2-YL]AMINO]-3-METHYL-1-BUTANOL

Description

Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. Purvalanol B is a CDK inhibitor that most potently inhibits Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p35, and Cdk2/cyclin B (IC₅₀s = 6, 9, 6, and 6 nM, respectively). It is inactive against Cdk4/cyclin D1 as well as several other protein kinases. Purvalanol B is a 2,6,9-trisubstituted purine that, at micromolar doses, inhibits the growth of parasites, including Plasmodium.

Uses

Purvalanol B is a potent cyclin-dependent kinase 2 (CDK2) inhibitor. These cyclin-dependent kinases play key roles in the regulation of the cell cycle and small molecules that inhibit these proteins have therapeutic potential against various proliferative and neurodegenerative disorders.

Uses

Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. Purvalanol B is a CDK inhibitor that most potently inhibits Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p35, and Cdk2/cyclin B (IC50s = 6, 9, 6, and 6 nM, respectively). It is inactive against Cdk4/cyclin D1 as well as several other protein kinases. Purvalanol B is a 2,6,9-trisubstituted purine that, at micromolar doses, inhibits the growth of parasites, including Plasmodium.

Definition

ChEBI: Purvalanol B is a purvalanol. It has a role as a protein kinase inhibitor.

Biological Activity

Cyclin-dependent kinase inhibitor. IC 50 values are 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively. Selective over a range of other protein kinases (IC 50 > 10,000 nM). Shown to have antiproliferative properties, mediated by p42/p44 MAPK.

storage

Store at +4°C