| Name | Fatostatin hydrobromide |
| Description | 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. |
| Cell Research | 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. |
| Animal Research | Animal Models: Obese (ob/ob) mice (C57BL/6J background). Formulation: 10% DMSO in PBS. Dosages: 30 mg/kg. Administration: intraperitoneal injection |
| In vitro | 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. |
| In vivo | 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | 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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| Keywords | Golgi | ob/ob | inhibit | Fatostatin hydrobromide | prostate | SREBP-mediated | cancer | mice | insulin-induced | adipogenesis | Fatostatin Hydrobromide | Fatty Acid Synthase (FASN) | gene | human | expression | Inhibitor | 125B11 |
| Inhibitors Related | Betulin | Ezetimibe | Trimetazidine dihydrochloride | Pyrazinamide | A-769662 | VY-3-135 | Orlistat | trans-Chalcone | TVB-3664 | L-Carnitine | Lycorine | FASN-IN-1 |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Metabolism Compound Library | Inhibitor Library | Lipid Metabolism Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
