| 货号 | 13562-5mg |
| 描述 | Sterol regulatory element binding proteins (SREBPs) are transcription factors that have pivotal roles in lipogenesis and fat metabolism.1 The activation of SREBPs requires escort to the Golgi by SREBP cleavage-activating protein (SCAP) followed by proteolytic release of SREBP from the Golgi.2 Fatostatin is an inhibitor of SREBP activation, preventing SCAP-mediated escort of either SREBP-1 or SREBP-2 to the Golgi (IC50 = 5.6 µM).3,4 This blocks constitutive SREBP-mediated gene expression in the human prostate cancer cell line DU145.3 Fatostatin prevents insulin-induced adipogenesis of 3T3-L1 cells as well as growth induced by insulin-like growth factor 1 in DU145 cells (IC50 = 0.1 µM).5 Through its actions on SCAP/SREBP-1, it inhibits high glucose-induced upregulation of TGF-β in primary rat mesangial cells.6 This compound also alters lipid metabolism in vivo, reducing hepatic fat accumulation in ob/obmice.3 |
| 别名 | 125B11; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Horton, J.D.,Goldstein, J.L., and Brown, M.S. SREBPs: Activators of the complete program of cholesterol and fatty acid synthesis in the liver. Journal of Clinical Investigation 109, 1125-1131 (2002). 2.Raghow, R.,Yellaturu, C.,Deng, X., et al. SREBPs: The crossroad of physiological and pathological lipid homeostasis. Trends in Endocrinology and Metabolism 19(2), 65-73 (2008). 3.Kamisuki, S.,Mao, Q.,Abu-Elheiga, L., et al. A small molecule that blocks fat synthesis by inhibiting the activation of SREBP. Chemistry & Biology 16, 882-892 (2009). 4.Kamisuki, S.,Shirakawa, T.,Kugimiya, A., et al. Synthesis and evaluation of diaryl thiazole derivatives that inhibit activation of sterol regulatory element-binding proteins. Journal of Medicinal Chemistry 54(13), 4923-4927 (2011). 5.Choi, Y.,Kawazoe, Y.,Murakami, K., et al. Identification of bioactive molecules by adipogenesis profiling of organic compounds. The Journal of Biological Chemisty 278(9), 7320-7324 (2003). 6.Uttarwar, L.,Gao, B.,Ingram, A.J., et al. SREBP-1 activation by glucose mediates TGF-ß upregulation in mesangial cells. American Journal of Physiology.Renal Physiology 302(3), F329-F341 (2012). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 375.3 |
| 分子式 | C18H18N2S • HBr |
| CAS号 | 298197-04-3 |
| 稳定性 | ≥ 2 years |
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