SR9243

SR9243 is a small molecule, selective, nanomolar inverse agonist of the liver X receptors (LXRα and LXRβ). Co-developed by Saint Louis University and The Scripps Research Institute, SR9243 selectively targets the Warburg effect and de novo lipogenesis in cancer cells. It works by enhancing LXR-corepressor recruitment, which suppresses the expression of key glycolytic and lipogenic genes (such as FASN, SREBF1, and SCD1). This metabolic disruption starves cancer cells of energy and vital lipids, inducing apoptosis in various cancer types (including colorectal, prostate, lung, and pancreatic cancers) without causing toxicity to normal cells. Additionally, SR9243 has shown preclinical efficacy in reducing intrahepatic inflammation and fibrosis in animal models of nonalcoholic steatohepatitis (NASH) and attenuating experimental rheumatoid arthritis.

Other names

N-(3-bromophenethyl)-2,4,6-trimethyl-N-((3'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)methyl)benzenesulfonamideN-(3-bromophenethyl)-2,4,6-trimethyl-N-((3'-(methylsulfonyl)biphenyl-4-yl)methyl)benzenesulfonamideN-[2-(3-bromophenyl)ethyl]-2,4,6-trimethyl-N-[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl]-benzenesulfonamide