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Sterol regulatory element binding proteins (SREBPs) are transcription factors that have pivotal roles in lipogenesis and fat metabolism. The activation of SREBPs requires escort to the Golgi by SREBP cleavage-activating protein (SCAP) followed by proteolytic release of SREBP from the Golgi. 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). This blocks constitutive SREBP-mediated gene expression in the human prostate cancer cell line DU145. 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). Through its actions on SCAP/SREBP-1, it inhibits high glucose-induced upregulation of TGF-beta in primary rat mesangial cells. This compound also alters lipid metabolism in vivo, reducing hepatic fat accumulation in ob/ob mice.Formal Name: 4-[4-(4-methylphenyl)-2-thiazolyl]-2-propyl-pyridine, hydrobromide. CAS Number: 298197-04-3. Synonyms: 125B11. Molecular Formula: C18H18N2S . HBr. Formula Weight: 375.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 1.25 mg/ml, Ethanol: 0.11 mg/ml. lambdamax: 257, 336 nm. SMILES: CC(C=C1)=CC=C1C2=CSC(C3=CC(CCC)=NC=C3)=N2.Br. InChi Code: InChI=1S/C18H18N2S.BrH/c1-3-4-16-11-15(9-10-19-16)18-20-17(12-21-18)14-7-5-13(2)6-8-14,/h5-12H,3-4H2,1-2H3,1H. InChi Key: RJCFNQZVFUMORB-UHFFFAOYSA-N.
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