Uses
Aminopurvalanol A is a reversible and ATP-competitive inhibitor of Cdks.
Definition
ChEBI: Aminopurvalanol is a purvalanol and a member of monochlorobenzenes. It has a role as a protein kinase inhibitor.
Biological Activity
Cell-permeable cyclin-dependent kinase inhibitor. IC 50 values are 0.033, 0.033, 0.028 and 0.020 μ M for cdk1/cyclin B, cdk2/cyclin A, cdk2/cyclin E, and cdk5/p35 respectively. Inhibits ERK1 (IC 50 = 12.0 μ M) and ERK2 (IC 50 = 3.1 μ M) and is 3000-fold selective over a range of other protein kinases (IC 50 > 100 μ M). Arrests cell cycle at G 2 /M boundary (IC 50 = 1.25 μ M), and induces apoptosis at concentrations > 10 μ M.
Enzyme inhibitor
This cell-permeable purvalanol derivative (FW = 403.92 g/mol), also named (2R)-2-[[6-[(3-Amino-5-chlorophenyl)amino]-9-(1-methylethyl)- 9H-purin-2-yl]amino]-3-methyl-1-butanol, targets cdk1/cyclin B (IC50 = 0.033 μM), cdk2/cyclin A (IC50 = 0.033 μM), cdk2/cyclin E (IC50 = 0.028 μM), and cdk5/p35 (IC50 = 0.020 μM). It also inhibits ERK1 (IC50 = 12 μM) and ERK2 (IC50 = 3.1 μM), with 3000-times greater selectivity versus a range of other protein kinases (IC50 > 100 μM). Aminopurvalanol A arrests cell cycle at G2/M boundary (IC50 = 1.25 μM), and induces apoptosis at concentrations > 10 μM.
