プロパティ

安全情報(bào)

説明

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-β in primary rat mesangial cells. This compound also alters lipid metabolism in vivo, reducing hepatic fat accumulation in ob/ob mice.