FGH10019

FGH10019 is an inhibitor of sterol regulatory element binding protein (SREBP) activation and a derivative of fatostatin (Item No. 13562).¹ It inhibits SREBP-mediated transcriptional activity in a reporter assay using CHO-K1 cells (IC₅₀ = 0.7 µM). FGH10019 increases plasma membrane fluidity and permeability in C4-2 and PC3 prostate cancer cells and has additive cytotoxic effects in the same cells when used in combination with docetaxel (Item No. 11637).² When administered with docetaxel, FGH10019 (20 mg/kg, p.o.) induces intratumoral apoptosis and reduces tumor volume in a PC3 mouse xenograft model in an additive manner. FGH10019 reduces body weight, serum levels of total and LDL cholesterol, hepatic levels of triglycerides, and blood glucose levels in ob/ob mice.¹

WARNING This product is not for human or veterinary use.

1. 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).

2. Chen, J., Wang, M.E., Bawcom, A.R., et al. Targeting SREBP-dependent lipogenesis potentiates the anti-tumor activity of docetaxel by increasing membrane permeability and intracellular drug accumulation. Oncogene 44(45), 4405-4412 (2025).