| 产品描述： | Fatostatin (125B11) 是一种diarylthiazole的衍生物，是 Sterol regulatory element binding proteins (SREBPs) 活化的特异性抑制剂。Fatostatin 可结合SCAP (SREBP cleavage-activating protein)，并抑制SREBP的ER-Golgi易位。Fatostatin 可抑制癌细胞生长并增强癌细胞的凋亡 |
| 靶点： |
SREBP;NPC1L1; FattyAcidSynthase |
| 体外研究： |
Fatostatin impairs the activation process of sterol regulatory element binding proteins (SREBPs), thereby decreasing the transcription of lipogenic genes in cells. Fatostatin inhibits the ER-Golgi translocation of SREBPs through binding to their escort protein, the SREBP cleavage-activating protein (SCAP), at a distinct site from the sterol-binding domain |
| 体内研究： |
Fatostatin blocks increases in body weight, blood glucose, and hepatic fat accumulation in obese ob/ob mice, even under uncontrolled food intake. Fatostatin may serve as a tool for gaining further insights into the regulation of SREBP |
| 细胞实验： |
Cell lines: CHO-K1 cells Concentrations: 20 μM Incubation Time: 20 h Method: CHO-K1 cells are plated out onto a 96-well plate in medium A. The cells are transiently cotransfected with pCMV-PLAP-BP2, pCMV-SCAP, and pAc-b-gal, using Lipofectamine reagent. After incubation for 5 hr, the cells are washed with PBS and then incubated in medium B, in the absence or presence of fatostatin (20 μM) or sterols (10 μg/mL cholesterol and 1 μg/mL 25-hydroxycholesterol). After 20 hr of incubation, an aliquot of the medium is assayed for secreted alkaline phosphatase activity. The cells in each well are lysed and used for measurement of b-galactosidase activities. The alkaline phosphatase activity is normalized by the activity of b-galactosidase. |
| 动物实验： |
Animal Models: 4-to-5-week-old homozygous male obese (ob/ob) mice (C57BL/6J) Dosages: 30 mg/kg Administration: IP |
| 参考文献： |
1. Shinji Kamisuki, et al. A small molecule that blocks fat synthesis by inhibiting the activation of SREBP. Chem Biol. 2009 Aug 28;16(8):882-92. 2. Shuhong Gao, et al. Fatostatin suppresses growth and enhances apoptosis by blocking SREBP-regulated metabolic pathways in endometrial carcinoma. Oncol Rep. 2018 Apr;39(4):1919-1929. |
| 溶解性： |
Soluble in DMSO、Ethanol |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.397 ml |
16.983 ml |
33.966 ml |
| 5 mM |
0.679 ml |
3.397 ml |
6.793 ml |
| 10 mM |
0.34 ml |
1.698 ml |
3.397 ml |
| 50 mM |
0.068 ml |
0.34 ml |
0.679 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京