XCT-790

XCT-790 is a potent and selective small-molecule inverse agonist of the orphan nuclear receptor Estrogen-Related Receptor alpha (ERRα). It functions by binding to the ligand-binding domain of ERRα, which leads to the recruitment of co-repressors and the subsequent proteasomal degradation of the receptor. ERRα is a key regulator of mitochondrial biogenesis, oxidative phosphorylation, and fatty acid oxidation. By inhibiting ERRα activity, XCT-790 has been shown to suppress the expression of genes involved in energy metabolism and has demonstrated anti-proliferative effects in various cancer cell lines, particularly those that are estrogen receptor-negative or overexpress ERRα. It was originally identified by GlaxoSmithKline and is widely utilized as a chemical probe in metabolic and oncological research.

Other names

3-[4-(2,4-bis-trifluoromethyl-benzyloxy)-3-methoxy-phenyl]-2-cyano-N-(5-trifluoromethyl-1,3,4-thiadiazol-2-yl)-acrylamide