Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.