Purvalanol-A-NG-60-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPurvalanol ACat. No.: HY-18299ACAS No.: 212844-53-6Synonyms: NG-60分式: CHClNO分量: 388.89作靶點: CDK; Autophagy作通路: Cell Cycle/DNA Damage; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO :

2、 50 mg/mL (128.57 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.43 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (6.43 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Purvalanol A種有效的 CDK 抑制劑，對 cdc2-cyclin

3、B，cdc2-cyclin B，cdk2-cyclin E，cdk4-cyclin D1 和cdk5-p35 的 IC50 值分別為 4，70，35，850 和 75 nM。IC50 & Target cdc2-cyclin B cdk2-cyclin E cdk2-cyclin A cdk4-cyclin D14 nM (IC50) 35 nM (IC50) 70 nM (IC50) 850 nM (IC50)cdk5-p35 erk175 nM (IC50) 9000 nM (IC50)體外研究 Purvalanol A inhibits cdc28 (S. cerevisiae) and

4、 erk1 with IC50s of 80 and 9000 nM. Purvalanol A showsinhibitory activities against the NCI panel of 60 human tumor cell lines, with average GI50 of 2 M; two celllines show an -20-fold increase in sensitivity to purvalanol A: the KM12 colon cancer cell line with a GI50 of76 nM and the NCI-H522 nonsm

5、all 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 kinasesin the low micromolar range. Purvalanol A inhibits MKK1, MAPK2/ERK2, JNK/SAPK1c with IC50s of 80, 26,84 M 2. Purval

6、anol A selectively inhibits the phosphorylation of cellular proteins. Purvalanol A prevents theincreases of the contents of cyclins D and E during serum-induced G1 phase progression. Purvalanol A doesnot inhibit transcription under cell-free conditions 3.戶使本產(chǎn)品發(fā)表的科研獻 iScience. 2018 Dec.See more custo

7、mer validations on HYPERLINK / www.MedChemEREFERENCES1. Gray NS, et al. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science. 1998 Jul24;281(5376):533-8.2. Bain J, et al. The specificities of protein kinase inhibitors: an update. Biochem J. 2003 Apr 1;371(Pt 1):199-204.3. Villerbu N, et al. Cellular effects of purvalanol A: a specific inhibitor of cyclin-dependent kinase activities. Int J Cancer. 2002 Feb20;97(6):761-9.McePdfHeightCaution: Product has not been fully validated for medical applications.For r