基本信息

产品描述

Purvalanol A 是一种有效的，细胞渗透性 CDK 抑制剂，对cdc2-cyclin B，cdk2-cyclin A，cdk2-cyclin E，和 cdk4-cyclin D1的 IC50 分别为 4 nM，70 nM，35 nM，和 850 nM。

靶点（IC50 & Targe）

Cdc2/CyclinB,4nM

CDK2/CyclinA,70nM

CDK2/CyclinE,35nM

CDK4/CyclinD1,850nM

体外研究

Purvalanol A剂量依赖性降低MCF-7和MDA-MB-231细胞系中细胞活性。Purvalanol A在MCF-7细胞中诱导50%的细胞活性损失，而MDA-MB-231细胞对Purvalanol A敏感性较低(细胞活性减少32 %)。Purvalanol A在MCF-7和MDA-MB-231细胞中诱导线粒体介导的细胞凋亡。[2] Purvalanol A通过抑制细胞周期进程和c-Src信号通路，有效防止c-Src介导转化，并有效抑制一些c-Src上调的人类癌细胞贴壁不依赖性生长。 Purvalanol A对HT29和SW480人结肠癌细胞的贴壁依赖性生长具有强烈的抑制作用。[3]

细胞实验

Cell lines: MCF-7和 MDA-MB 231乳腺癌细胞

Concentrations: 100 μM

Incubation Time: 24 h

Method: 细胞以10000的密度接种于96孔板，并用不同浓度的Purvalanol A (0-100 μM)处理24小时。细胞暴露于10 μL MTT染料(5 mg/mL)，并在37℃下培养4小时。为溶解甲瓒晶体，加入100 μL DMSO。吸光度在570 nm分光光度法测定。

(Only for Reference)

参考文献

[1] Gray NS, et al. Science. 1998, 281(5376), 533-538.

[2] Obakan P, et al. Mol Biol Rep. 2014, 41(1), 145-154.

[3] Hikita T, et al. Genes Cells. 2010, 15(10), 1051-1062.

产品说明

一般描述

A potent, cell-permeable, reversible, and selective inhibitor of cyclin-dependent kinases (Cdks; IC₅₀ = 4 nM for Cdc2-cyclin B; IC₅₀ = 70 nM for Cdk2-cyclin A; IC₅₀ = 35 nM for Cdk2-cyclin E; and IC₅₀ = 75 nM for Cdk5-p35).
A potent, cell-permeable, reversible, and selective inhibitor of cyclin-dependent kinases (Cdks; IC₅₀ = 4 nM for Cdc2/cyclin B; IC₅₀ = 70 nM for Cdk2/cyclin A; IC₅₀ = 35 nM for Cdk2/cyclin E; and IC₅₀ = 75 nM for Cdk5/p35).

包装

1 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Product does not compete with ATP.
Primary Target
Cdc2/cyclin B
Reversible: yes
Cell permeable: yes
Target IC₅₀: 4 nM for Cdc2/cyclin B; 70 nM for Cdk2/cyclin A; 35 nM for Cdk2/cyclin E; 75 nM for Cdk5/p35

警告

Toxicity: Standard Handling (A)

重悬

Following initial thaw, aliquot and freeze (-20°C).

其他说明

Gray, N.S., et al. 1998. Science 281, 533.

法律信息

Sold under license of U.S. Patents 6,617,331 and 6,803,371.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

产品性质

安全信息

产品说明

包装

1 mg in glass bottle

生化/生理作用

Purvalanol A is found to inhibit ABCG2 (ATP-binding cassette G2) transporter in vitro. It is also known to attenuate cellular Src kinase action and induce cell cycle arrest at the G2 to M phase transition.
Purvalanol A is a potent, cell-permeable cyclin-dependent protein kinase (cdk) inhibitor.

特点和优势

This compound is featured on the CDKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

基本信息

产品性质

安全信息

基本信息