Chemical Name |
Purvalanol A |
CAS Number |
212844-53-6 |
MDL Number |
MFCD02179211 |
Molecular Formula |
C19H25ClN6O |
Molecular Weight |
388.89 |
Synonyms |
NG-60 |
Introduction of 212844-53-6 :
Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively. IC50 & Target: IC50: 4 nM (cdc2-cyclin B), 70 nM (cdk2-cyclin A), 35 nM (cdk2-cyclin E), 850 nM (cdk4-cyclin D1), 75 nM (cdk5-p35)[1] In Vitro: 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[1]. 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[2]. 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[3].
Purity |
NLT 98% |
Storage |
at 20ºC 2 years |
*The above information is for reference only.