Fatostatin (hydrobromide)

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).^1,2 This blocks constitutive SREBP-mediated gene expression in the human prostate cancer cell line DU145.¹ 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).³ Through its actions on SCAP/SREBP-1, it inhibits high glucose-induced upregulation of TGF-β in primary rat mesangial cells.⁴ This compound also alters lipid metabolism in vivo, reducing hepatic fat accumulation in ob/ob mice.¹

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1. Kamisuki, S., Mao, Q., Abu-Elheiga, L., et al. A small molecule that blocks fat synthesis by inhibiting the activation of SREBP. Chem. Biol. 16(8), 882-892 (2009).

2. Kamisuki, S., Shirakawa, T., Kugimiya, A., et al. Synthesis and evaluation of diaryl thiazole derivatives that inhibit activation of sterol regulatory element-binding proteins. J. Med. Chem. 54(13), 4923-4927 (2011).

3. Choi, Y., Kawazoe, Y., Murakami, K., et al. Identification of bioactive molecules by adipogenesis profiling of organic compounds. The Journal of Biological Chemisty 278(9), 7320-7324 (2003).

4. Uttarwar, L., Gao, B., Ingram, A.J., et al. SREBP-1 activation by glucose mediates TGF-ß upregulation in mesangial cells. Am. J. Physiol. Renal Physiol. 302(3), F329-F341 (2012).