半岛bd体育手机客户端 说明
一般描述
A cell-permeable diarylthiazole compound that prevents the cellular activation of the SREBP-1/2 (Sterol Regulatory Element Binding Proteins 1/2) precursors to the active nuclear forms (>95% inhibition at 20 ?M in CHO-K1 cells) by blocking SREBPs-SCAP (SREBP Cleavage-Activating Protein) ER to Golgi translocation with little effect against the transcription activity of the mature SREBPs. Binding studies employing recombinant SCAP truncation constructs reveal that Fatostatin targets SCAP between aa 448 to 767 in a reversible manner and is of no effect against SREBP-SCAP interaction. Fatostatin effectively suppresses SREBPs-dependent cellular functionsin vitro, such as insulin-induced 3T3-L1 adipogenesis (complete inhibition at ≤20 ?g/ml) and IGF1-dependent DU-145 proliferation (IC50= 100 nM), and exhibitsin vivoefficacy in lowering blood glucose level (by 70%) and body weight (by 12%) ofob/obmice over a 28-day treatment period (30 mg/kg daily i.p.) without affecting animal food intake or apparent adverse effects.
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Kamisuki, S., et al. 2009.Chem. Biol.16,882.
Choi, Y., et al. 2003.J. Biol. Chem.278,7320.
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 | C18H18N2S · xHBr |
| 分子量 | 294.41 (free base basis) |
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 desiccated (hygroscopic) protect from light |
| 颜色 | pale yellow |
| 溶解性 | DMSO: 10 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 1 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
Sigma-Aldrich
m.cnreagent.com
