半岛bd体育手机客户端 说明
一般描述
A cell-permeable thiazole-containing urea compound that acts as a potent inhibitor of GSK-3. Shown to inhibit GSK-3β with high potency (IC50= 104 nM). Inhibition is competitive with respect to ATP (Ki= 38 nM). Specificity has been reported using a panel of 28 different kinases, including Cdk2 and Cdk5 (IC50>100 ?M). Shown to prevent tau phosphorylation at a GSK-3-specific site. Also shown to protect neuronal cells against Aβ-mediated neurodegenerationin vitroand reduce tauopathy in micein vivo(30 ?mol/kg delivered with 40% PEG400 and 40% dimethylacetamide in water). Caution: Do not use delivering vehicles containing dimethylamine forin vivostudies, as it is highly toxic to animals. A 25 mM (5 mg/649 ?l) solution of GSK-3β Inhibitor VIII (Cat. No. 361557) in DMSO is also available.
A cell-permeable, potent inhibitor of glycogen synthase kinase-3 (GSK-3). Shown to inhibit GSK-3β with high potency (IC50= 104 nM). Inhibition is competitive with respect to ATP (Ki= 38 nM). Specificity has been reported using a panel of 28 different kinases, including Cdk2 and Cdk5 (IC50>100 ?M). Shown to prevent tau phosphorylation at a GSK-3-specific site. Also shown to protect neuronal cells against Aβ-mediated neurodegenerationin vitroand reduce tauopathy in micein vivo(30 ?mol/kg delivered with 40% PEG400 and 40% dimethylacetamide in water). Caution: Do not use delivering vehicles containing dimethylamine forin vivostudies, as it is highly toxic to animals.
包装
5 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Target IC50: 104 nM against GSK-3β
Primary Target
Gsk-3β
Reversible: no
Product competes with ATP.
警告
Toxicity: Carcinogenic / Teratogenic (D)
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
Noble, W., et al. 2005.Proc. Natl. Acad. Sci. USA102,6990.
Bhat, R., et al. 2003.J. Biol. Chem.278,45937.
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 | C12H12N4O4S |
| 分子量 | 308.31 |
| MDL编号 | MFCD08277040 |
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 | yellow |
| 溶解性 | DMSO: 5 mg/mL |
| 运输 | ambient |
| 储存温度 | 2-8℃ |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
Sigma-Aldrich
m.cnreagent.com
