FatoSTATin A 是一种SREBP活化的特异性抑制剂，能够抑制 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。它具有抗肿瘤活性，能抑制ob/ob小鼠的高血糖。它抑制细胞中成脂基因的转录。

Fatostatin is a specific inhibitor of SREBP activation, it 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 directly binds SCAP and blocks its ER-to-Golgi transport with IC50 of 2.5 and 10 μM in mammalian cells[1]. Fatostatin (0.1-1 μM; 3 days) inhibits the androgen-independent prostate cancer cell proliferation (IC50=0.1 μM) in an independent of the known IGF1-signaling pathway. Fatostatin inhibits insulin-induced adipogenesis of 3T3-L1 cells[2].

Fatostatin (30 mg/kg; i.p. injection; daily for 28 days) reduces adiposity, ameliorated fatty liver by reducing triglyceride (TG) storage, and lowered hyperglycemia in ob/ob mice[1].

125256-00-0

C18H18N2S

294.42

DMSO:70 mg/mL (237.76 mM)
H2O:Insoluble
Ethanol:70 mg/mL (237.76 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years