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Fatostatin hydrobromide (Fatostatin A HBr) 是一种 SREBP 活化的特异性抑制剂,可抑制 SREBP-1 和 SREBP-2 的活化。它与 SCAP (SREBP 裂解激活蛋白) 结合,抑制 SREBPs 的 ER-Golgi 易位。它具有抗肿瘤作用,能抑制 ob/ob 小鼠的高血糖。它抑制了细胞中成脂基因的转录。
Fatostatin hydrobromide (Fatostatin A HBr) 是一种 SREBP 活化的特异性抑制剂,可抑制 SREBP-1 和 SREBP-2 的活化。它与 SCAP (SREBP 裂解激活蛋白) 结合,抑制 SREBPs 的 ER-Golgi 易位。它具有抗肿瘤作用,能抑制 ob/ob 小鼠的高血糖。它抑制了细胞中成脂基因的转录。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 196 | 现货 | |
5 mg | ¥ 453 | 现货 | |
10 mg | ¥ 659 | 现货 | |
25 mg | ¥ 1,190 | 现货 | |
50 mg | ¥ 1,980 | 现货 | |
100 mg | ¥ 3,120 | 现货 | |
200 mg | ¥ 4,680 | 现货 | |
500 mg | ¥ 6,970 | 现货 |
产品描述 | Fatostatin hydrobromide (Fatostatin A HBr) ia an inhibitor of sterol regulatory element binding protein (SREBP). It impairs the activation of SREBP-1 and SREBP-2. |
体外活性 | Fatostatin inhibits the insulin-induced adipogenesis of 3T3-L1 cells and the serum-independent growth of human androgen-independent prostate cancer (DU145) cells. Fatostatin suppresses cell proliferation and anchorage-independent colony formation in both androgen-responsive LNCaP and androgen-insensitive C4-2B prostate cancer cells. Fatostatin blocks the activation of SREBPs in cells in tissue culture.Fatostatin also reduced in vitro invasion and migration in both cell lines. Further, fatostatin causes G2/M cell cycle arrest and induces apoptosis by increasing caspase-3/7 activity and the cleavages of caspase-3 and PARP. |
体内活性 | Fatostatin significantly inhibits subcutaneous C4-2B tumor growth and markedly decreases serum PSA level compared to the control group. Fatostatin blocks increases in body weight, blood glucose, and hepatic fat accumulation in obese ob/ob mice, even under uncontrolled food intake. |
细胞实验 | Cell lines: CHO-K1 cells. Concentrations: 20 μM. Incubation Time: 20 h. Method: On day 0,CHO-K1 cells are plated out onto a 96-well plate in medium A.On day 2,the cells are transiently cotransfected with pCMV-PLAP-BP2(513–1141),pCMV-SCAP,and pAc-β-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 β-galactosidase activities.The alkaline phosphatase activity is normalized by the activity of β-galactosidase. |
动物实验 | Animal Models: Obese (ob/ob) mice (C57BL/6J background). Formulation: 10% DMSO in PBS. Dosages: 30 mg/kg. Administration: intraperitoneal injection |
别名 | Fatostatin HBr, Fatostatin A HBr, Fatostatin A, Fatostatin |
分子量 | 375.33 |
分子式 | C18H18N2S·HBr |
CAS No. | 298197-04-3 |
Smiles | Br.CCCc1cc(ccn1)-c1nc(cs1)-c1ccc(C)cc1 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 3.75 mg/mL (10 mM), Sonication is recommended. Ethanol: 58 mg/mL (154.53 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||||||||||||||||||||||
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