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Aminopurvalanol A
Other Information:
Sold under licence from the Regents of the University
of California
Chemical Name:(2R)-2-[[6-[(3-Amino-5-chlorophenyl)amino]-9-(1-methyle
thyl)-9H-purin-2-yl]amino]-3-methyl-1-butanol
Biological Activity:
Cell-permeable cyclin-dependent kinase
inhibitor. IC50 values are 0.033, 0.033, 0.028 and 0.020 μM for
cdk1/cyclin B, cdk2/cyclin A, cdk2/cyclin E, and cdk5/p35 respectively.
Inhibits ERK1 (IC50 = 12.0 μM) and ERK2
(IC50 = 3.1 μM)
and is 3000-fold selective over a range of other protein kinases (IC50
> 100 μM).
Arrests cell cycle at G2/M boundary (IC50 = 1.25 μM), and
induces apoptosis at concentrations > 10 μM.
Changet al
(1999) Synthesis and application of functionally diverse 2,6,9-trisubstituted
purine libraries as CDK inhibitors. Chem.Biol. 6 361. Rosianaet al (1999) A cyclin-dependent kinase inhibitor inducing cancer cell
differentiation: biochemical identification using Xenopus egg extracts.
Proc.Natl.Acad.Sci.USA 96 4797. Knockaertet al
(2000) Intracellular targets of cyclin-dependent kinase inhibitors: identification
by affinity chromatography using immobilised inhibitors. Chem.Biol. 7
411.