5-bromo-5'-phenyl-1,2',3,3'-tetrahydrospiro[2H-indole-3,2'-(1,3,4)-thiadiazole]-2-one

Lipofermata (297180-15-5) is an inhibitor of fatty acid transport protein 2 (FATP2; IC50= 4.84 μM).1It does not inhibit glucose transport or the activity of long chain acyl-CoA synthetase. It prevented palmitate-mediated oxidative stress, induction of BiP and CHOP, and cell death in a dose-dependent manner in hsHepG2 and mINS-1E cells suggesting utility in preventing fatty acid-mediated cell death pathways and lipotoxic disease.2Inhibition was specific for long and very long chain fatty acids but not medium (C6-C10) acids. Lipofermata abrogates lipid transport into melanoma cells and reduces melanoma growth and invasion.3

Lipofermata is a fatty acid transport proteins (FATPs) inhibitor.

[1] ANGEL SANDOVAL . Identification and characterization of small compound inhibitors of human FATP2[J]. Biochemical pharmacology, 2010, 79 7: Pages 990-999. DOI:10.1016/j.bcp.2009.11.008
[2] CONSTANCE AHOWESSO . Chemical inhibition of fatty acid absorption and cellular uptake limits lipotoxic cell death[J]. Biochemical pharmacology, 2015, 98 1: Pages 167-181. DOI:10.1016/j.bcp.2015.09.004
[3] MAOMAO ZHANG. Adipocyte-Derived Lipids Mediate Melanoma Progression via FATP Proteins.[J]. Cancer discovery, 2018, 8 8: 1006-1025. DOI:10.1158/2159-8290.cd-17-1371