产品说明
一般描述
A cell-permeable aminopyrimidine compound that acts as potent, ATP-competitive, and highly selective GSK-3 inhibitor (IC50 = 10 and 6.7 nM against GSK-3α and GSK-3β, respectively). Exhibits little or no activity toward 46 other enzymes (IC50 >8.8 µM against 20 kinases and Ki ≥5 µM against 23 non-kinase enzymes) and shows only weak binding to 22 pharmacologically relevant receptors (Kd ~4 µM). This compound is orally available and is shown to effectively improve glucose metabolism in both murine and rat type 2 diabetes models in vivo. The solid form of this compound (Cat. No. 361559) is also available.
包装
5 mg in Glass bottle
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Primary Target
GSK-3 α and β
Reversible: yes
Target IC50: 10 and 6.7 nM against GSK-3&alpha
警告
Toxicity: Irritant (B)
外形
A 25 mM (5 mg/430 µL) solution of GSK-3 Inhibitor XVI, CHIR99021 (Cat. No. 361559) in DMSO.
其他说明
Mussmann, R., et al. 2007. J. Biol. Chem.282, 12030.
Ring, D.B., et al. 2003. Diabetes52, 588.
Bennett, C.N., et al. 2002. J. Biol. Chem.277, 30998.
Cline, G.W., et al. 2002.
Diabetes51, 2903.
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 | C22H18Cl2N8 |
| 分子量 | 465.34 |
| MDL编号 | MFCD11846251 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥95% (HPLC) |
| 形式 | liquid |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze avoid repeated freeze/thaw cycles desiccated (hygroscopic) protect from light |
| 运输 | ambient |
| 储存温度 | −70℃ |
安全信息
| 储存分类代码 | 10 - Combustible liquids |
| WGK | WGK 2 |
| 闪点(F) | 188.6 °F - (refers to pure substance) |
| 闪点(C) | 87 ℃ - (refers to pure substance) |
