A selective CDK inhibitor; inhibits Cdk1/cyclin B

Aminopurvalanol A – 5 mg

Brand:
Cayman
CAS:
220792-57-4
Storage:
-20
UN-No:
Non-Hazardous - /

Aminopurvalanol A is a selective, cell-permeable, and competitive cyclin-dependent kinase (CDK) inhibitor that potently inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p35 (IC50s = 33, 33, 28, and 20 nM, respectively).{39089} It is over 90-fold selective for CDKs over ERK1, ERK2, PKC-δ, protein kinase A (PKA), casein kinase 1, insulin receptor tyrosine kinase (IC50s = 3.0-36 μM), and over 3,000-fold selective over a range of other kinases (IC50s > 100 μM). In antiproliferative assays in vitro, aminopurvalanol A inhibits growth of ovarian (IGROV1), leukemic (SR), lung (NCI-H522), and colonic (KM12) cells (GI50s = 470, 420, 1,000, and 30 nM, respectively). Aminopurvalanol A also inhibits mitotic division and preferentially arrests cells in the G2/M phase via Cdk1/cyclin B{39090,39091}  

 

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Description

A selective CDK inhibitor; inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p35 (IC50s = 33, 33, 28, and 20 nM, respectively); 90-fold selective for CDKs over ERK1, ERK2, PKC-δ, PKA, CK1, and insulin receptor tyrosine kinase; over 3,000-fold selective over a range of other kinases; antiproliferative (GI50s = 30-1,000 nM); inhibits mitotic division; preferentially arrests cells in G2/M phase

Formal name: (2R)-2-[[6-[(3-amino-5-chlorophenyl)amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-3-methyl-1-butanol

Synonyms:  NG 97

Molecular weight: 403.9

CAS: 220792-57-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|CDKs||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Signaling

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