半岛bd体育手机客户端 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 remarkablein vitroantitumor 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 activityin vitro. Inhibits growth of the colon cancer cell line HCT-116, with an IC50in 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
经验(实验)分子式 | C16H11N3O3 |
分子量 | 293.28 |
MDL编号 | MFCD02683579 |
半岛bd体育手机客户端 性质
质量水平 | 100 |
测定 | ≥95% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem? |
储存条件 | OK to freeze protect from light |
颜色 | light yellow to brown |
溶解性 | DMSO: 20 mg/mL |
运输 | ambient |
储存温度 | ?20℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
Sigma-Aldrich