产品说明

一般描述

A cell-permeable, potent, reversible, and ATP competitive inhibitor of GSK-3β (IC₅₀ = 4 nM) and Cdk1/cyclin B (IC₅₀ = 35 nM). Displays remarkable in vitro antitumor activity. Inhibits Tau phosphorylation at sites that are typically phosphorylated by GSK-3β in Alzheimer’s disease. Also inhibits Cdk5/p25-dependent phosphorylation of DARPP-32.
A cell-permeable, potent, reversible, and ATP competitive inhibitor of cdk1/cyclin B (IC₅₀ = 35 nM) and GSK-3β (IC₅₀ = 4 nM). One of the most active paullones that acts by competing with ATP for binding to GSK-3β and inhibits the phosphorylation of tau. Also inhibits the activity of Cdk5/p25-dependent phosphorylation of DARPP-32 (a 32 kDa dopamine and adenosine 3′,5′-monophosphate-regulated phosphoprotein). Displays remarkable antitumor activity in vitro. Inhibits growth of the colon cancer cell line HCT-116, with an IC₅₀ in the nanomolar range.

包装

1 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Target IC₅₀: 4 nM, 35 nM, against GSK-3β, Cdk1/cyclin B, respectively
Product competes with ATP.
Reversible: yes
Primary Target
GSK-3β, Cdk1/cyclin B

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Leost, M., et al. 2000. Eur. J. Biochem.267, 5983.
Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.

法律信息

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

应用

Alsterpaullone 已用于稳定 β-catenin。
Alsterpaullone 抑制 GSK-3β、CDK5/p25 和 CDK1/cyclinB。Alsterpaullone 也已被作为抗躁狂药进行研究，用于双相情感障碍急性躁狂期的治疗。

包装

1 mg in glass bottle

生化/生理作用

Alsterpaullone(ALP)是一种细胞周期蛋白依赖性激酶(CDK)抑制剂。它被认为是第 3 组髓母细胞瘤的治疗药物。Alsterpaullone 调节细胞周期的进程。它可以通过干扰线粒体膜电位来激活 caspase-9，从而阻止细胞周期并刺激癌细胞凋亡。
GSK-3β 和 CDK5/p25; 的有效和选择性抑制剂；CDK1/cyclin B 的有效抑制剂(IC₅₀ = 0.035 μM)。

特点和优势

该化合物出现在受体分类和信号转导手册的 CDKs 和 GSK-3页。欲浏览其他手册页，点击此处。

基本信息

产品性质

安全信息