Purvalanol A

Research use only, not for human use.

A potent, cell-permeable, selective inhibitor of CDK with IC50s of 4, 70, 35, 850, and 75 nM for cdc2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk4/cyclin D1 and Cdk5-p35, respectively.

A potent, cell-permeable, selective inhibitor of CDK with IC50s of 4, 70, 35, 850, and 75 nM for cdc2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk4/cyclin D1 and Cdk5-p35, respectively; also inhibits Saccharomyces cerevisiae Cdc28p (IC50=80 nM) and has no effect on PKC, Raf, CK1, CK2.

Purvalanol A inhibits cdc28 (S. cerevisiae) and erk1 with IC50s of 80 and 9000 nM. Purvalanol A shows inhibitory activities against the NCI panel of 60 human tumor cell lines, with average GI50 of 2 μM; two cell lines show an -20-fold increase in sensitivity to purvalanol A: the KM12 colon cancer cell line with a GI50 of 76 nM and the NCI-H522 non–small cell lung cancer cell line with a GI50 of 347 nM. Purvalanol A is a 2.5-fold more potent inhibitor of CDK2, but also inhibits DYRK1A potently and a number of other protein kinases in the low micromolar range. Purvalanol A inhibits MKK1, MAPK2/ERK2, JNK/SAPK1c with IC50s of 80, 26, 84 μM. Purvalanol A selectively inhibits the phosphorylation of cellular proteins. Purvalanol A prevents the increases of the contents of cyclins D and E during serum-induced G1 phase progression. Purvalanol A does not inhibit transcription under cell-free conditions.

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NG-60 | NG 60 | NG60

Angiogenesis

CDK

Cdc2/CyclinB|CDK2/CyclinA|CDK2/CyclinE|CDK4/CyclinD1

Cancer

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212844-53-6

388.8944

C19H25ClN6O

>98% (HPLC)

10 mM in DMSO

CC(C)[C@@H](NC1=NC(NC2=CC=CC(Cl)=C2)=C3N=CN(C(C)C)C3=N1)CO

1-Butanol, 2-[[6-[(3-chlorophenyl)amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-3-methyl-, (2R)-

(-20℃)

With Ice Pack

≥ 2 years