product name Purvalanol A
Description: Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively. In MKN45 cells, purvalanol A (30 μM) reduced the expression of antiapoptotic proteins Bcl-2, Bcl-XL and survivin and induced apoptosis. Also, purvalanol A inhibited the phosphorylation of STAT3 by Janus kinase 2 (JAK2) and the expression and phosphorylation of RNA polymerase II, which was involved in transcriptional regulation.
References: Science. 1998;281(5376):533-8; Mol Biol Rep. 2014;41(1):145-54; Genes Cells. 2010;15(10):1051-62.
388.89
Formula
C19H25ClN6O
CAS No.
212844-53-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 60 mg/mL (154.3 mM)
Water: <1 mg/mL
Ethanol: 13 mg/mL (33.4 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19405902
| In Vitro |
In vitro activity: Purvalanol A decreases cell viability in dose-dependent manner in MCF-7 and MDA-MB-231 cell lines. Purvalanol A induces cell viability loss by 50 % in MCF-7 cells but MDA-MB-231 cells sre less sensitive to Purvalanol A (32 % decreases in cell viability). Purvalanol A induces mitochondria-mediated apoptosis in MCF-7 and MDA-MB-231 cells. Purvalanol A effectively prevents c-Src-mediated transformation by inhibiting both cell cycle progression and c-Src signaling, and effectively suppresses the anchorage independent growth of some human cancer cells in which c-Src is up-regulated. Purvalanol A has a stronger inhibitory effect on the anchorage-independent growth of HT29 and SW480 human colon cancer cells. Kinase Assay: Cell Assay: Cells are seeded at 10000 density in 96-well plates and treated with various concentrations of Purvalanol A (0-100 μM) for 24 h. Cells are exposed to 10 μL of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltet- razolium bromide dye (5 mg/mL) and are incubated at 37℃ for 4 h. In order to solubilize the formazan crystals 100 μL DMSO is added. Absorbance is determined at 570 nm spectrophotometrically. |
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| In Vivo | In the dentate gyrus (DG) of the rat hippocampus, purvalanol A (40 nmol/3 μl) significantly induced the number of BrdU-positive cells in a time- and concentration-dependent way. |
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| Formulation & Dosage | |
| References | Science. 1998 Jul 24;281(5376):533-8; Mol Biol Rep. 2014 Jan;41(1):145-54; Genes Cells. 2010 Oct;15(10):1051-62. |
