(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

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] M KNOCKAERT. Intracellular targets of cyclin-dependent kinase inhibitors: identification by affinity chromatography using immobilised inhibitors.[J]. Chemistry & biology, 2000, 7 6: 411-422. DOI: 10.1016/s1074-5521(00)00124-1
[3] KRISTEN M BULLARD  Susan M K  Carolyn Broccardo. Effects of cyclin-dependent kinase inhibitor Purvalanol B application on protein expression and developmental progression in intra-erythrocytic Plasmodium falciparum parasites.[J]. Malaria Journal, 2015: 147. DOI: 10.1186/s12936-015-0655-x