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Purvalanol A
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Purvalanol A图片
CAS NO:212844-53-6
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
25mg电议
100mg电议

产品介绍
Purvalanol A 是一种有效的 CDK 抑制剂，可分别抑制 cdc2-cyclin B、cdk2-cyclin A、cdk2-cyclin E、cdk4-cyclin D1 和 cdk5-p35，IC50 分别为 4、70、35、850、75 nM。
Cas No.212844-53-6
别名NG-60
化学名(R)-2-((6-((3-chlorophenyl)amino)-9-isopropyl-9H-purin-2-yl)amino)-3-methylbutan-1-ol
Canonical SMILESClC1=CC(NC2=C3C(N(C(C)C)C=N3)=NC(N[C@@H](CO)C(C)C)=N2)=CC=C1
分子式C19H25ClN6O
分子量388.89
溶解度≥ 19.45mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Purvalanol A is a potent and selective inhibitor of CDK with IC50 values of 4, 35, 70, 75 and 850 nM for cdc2-cyclin B, cdk2-cyclin E, cdk2-cyclin A, cdk5-p35 and cdk4-cyclin D1, respectively [1].

Cyclin-dependent kinases (CDKs) are a family of protein kinases and play an important role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells.

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 [2]. In MCF-7 ER(+) cells, purvalanol A induced apoptosis in a caspase-dependent way and increased the levels of spermidine/spermine N1-acetyltransferase (SSAT) and polyamine oxidase (PAO) [3].

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 [4].

References:
[1].  Gray NS, Wodicka L, Thunnissen AM, et al. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science, 1998, 281(5376): 533-538.
[2].  Iizuka D, Ogura A, Kuwabara M, et al. Purvalanol A induces apoptosis and downregulation of antiapoptotic proteins through abrogation of phosphorylation of JAK2/STAT3 and RNA polymerase II. Anticancer Drugs, 2008, 19(6): 565-572.
[3].  Obakan P, Ar?san ED, ?zfiliz P, et al. Purvalanol A is a strong apoptotic inducer via activating polyamine catabolic pathway in MCF-7 estrogen receptor positive breast cancer cells. Mol Biol Rep, 2014, 41(1): 145-154.
[4].  Ma?kowiak M, Kolasiewicz W, Markowicz-Kula K, et al. Purvalanol A, inhibitor of cyclin-dependent kinases attenuates proliferation of cells in the dentate gyrus of the adult rat hippocampus. Pharmacol Rep, 2005, 57(6): 845-849.