产品说明
一般描述
A cell-permeable triaryl substituted imidazolo compound that acts as a potent, reversible and relatively specific ATP-competitive inhibitor of CK1 (IC50 = 0.2 µM from S. pombe; 0.3 µM for CK1δ) and ALK5 (IC50 = 0.5 µM). A weak inhibitor of p38α MAP kinase (IC50 = 12 µM) and only weakly affects the activities of a panel of kinases tested, including PKB, SGK and GSK-3β. Suppresses the site-specific phosphorylation (Ser322 and Ser325) and nuclear exclusion of FOXO1a in H4IIE hepatoma cells. Shown to be ~10-fold more potent than IC261 (Cat. No. 400090; IC50 = 2.5 µM for CK1).
A cell-permeable, reversible, potent, and relatively specific ATP-competitive inhibitor of CK1 (IC50 = 200 nM from S. pombe; 0.3 µM for CK1δ) and ALK5 (IC50 = 500 nM). A weak inhibitor of p38α MAP kinase (IC50 = 12 µM) and several other kinases tested, including PKB, SGK, and GSK-3β. Suppresses the site-specific phosphorylation (Ser322 and Ser325) and nuclear exclusion of FOXO1A in H4IIE hepatoma cells. Shown to be ~ 10-fold more potent than IC261 (Cat. No. 400090; IC50 = 2.5 µM for CK1).
包装
1 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Target IC50: 0.2 µM against CK1 from S. pombe; 0.3 µM for CK1δ 0.5 µM against ALK5
Product competes with ATP.
Reversible: yes
警告
Toxicity: Standard Handling (A)
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 | C23H18N4O3 |
分子量 | 398.41 |
产品性质
质量水平 | 100 |
测定 | ≥95% (HPLC) |
形式 | crystalline solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
溶解性 | DMSO: 40 mg/mL |
运输 | ambient |
储存温度 | 2-8℃ |
Sigma-Aldrich