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CAS No.: 212844-53-6

Purvalanol A Catalog No. CSN11800

Synonyms: NG-60;Purv

Purvalanol A is a selective inhibitor of cyclin-dependent kinases (CDKs), it potently inhibits cdc2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk4/cyclin D1 and Cdk5-p35 with IC50 values of 4, 70, 35, 850, and 75 nM respectively.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述CDK2 is a serine/threonine-protein kinase involved in the control of the cell cycle; essential for meiosis, but dispensable for mitosis. CDK2 triggers duplication of centrosomes and DNA, acts at the G1-S transition to promote the E2F transcriptional program and the initiation of DNA synthesis, and modulates G2 progression. CDK2 controls the timing of entry into mitosis/meiosis by controlling the subsequent activation of cyclin B/CDK1 by phosphorylation, and coordinates the activation of cyclin B/CDK1 at the centrosome and in the nucleus. Purvalanol A is a CDK2 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, respectively. Based on kinase assays performed in immunoprecipitates, the IC50s of purvalanol A against 2 yeast CDKs (Cdc28p and Pho85p) were 7 μM and 2 μM, respectively^[3]. According to a MTT cell viability assay, purvalanol A induced cell viability loss by 50% in MCF-7 cells at the concentration of 25 μM when incubated in vitro for 24h^[4].In a spinal cord injury model established in Sprague–Dawley rats, 5 μl of purvalanol A at the concentration of 10 mM in DMSO was immediately injected into the injury site. The results were that purvalanol A restricted compaction of the injury cavity and astrocyte infiltration into the cavity. Purvalanol A treatment also attenuated regenerative responses of anterogradely labeled corticospinal tract axons. Moreover, purvalanol A treatments reduced astrocyte migration and in parallel retarded the extension of spinal axon, observed by the technique of implantation of a polymeric tube into the spinal cord^[5].
作用机制Purvalanol A is a CDK2 inhibitor that acts by blocking the ATP-binding site^[3].
动物研究
剂量
Mice: 30 mg/kg^[3] (i.v.)

给药途径
i.v.
参考文献

动物研究
剂量	Mice: 30 mg/kg^[3] (i.v.)
给药途径	i.v.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5714 mL
- 12.8570 mL
- 25.7139 mL
- 5 mM
- 0.5143 mL
- 2.5714 mL
- 5.1428 mL
- 10 mM
- 0.2571 mL
- 1.2857 mL
- 2.5714 mL

技术信息

CAS号

212844-53-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H25ClN6O

运输

蓝冰

分子量

388.89

别名

NG-60;Purv

溶解度

DMSO	50.0 mg/mL (128.6 mM)
Water	insoluble

动物实验配方

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