ERG-240

ERG-240 is a small molecule leucine analog that acts as a selective inhibitor of branched-chain aminotransferase 1 (BCAT1). Developed by Ergon Pharmaceuticals, ERG-240 blocks the transamination of branched-chain amino acids (BCAAs) like leucine, which is a key step in metabolic reprogramming. In cancer cells, BCAT1 inhibition by ERG-240 suppresses cell proliferation, migration, and the expression of prometastatic proteins such as CD147 and monocarboxylate transporter-4 (MCT-4). In inflammatory contexts, ERG-240 has been shown to reprogram macrophages, reducing oxygen consumption, glycolysis, and itaconate production via the IRG1/itaconate axis. Preclinical studies have demonstrated its efficacy in reducing inflammation and disease severity in animal models of rheumatoid arthritis, crescentic glomerulonephritis, and vulnerable atherosclerotic plaques.

Other names

4-methyl-5-oxohexanoic acid sodium saltsodium 4-methyl-5-oxohexanoatesodium4-methyl-5-oxohexanoatesodium-4-methyl-5-oxohexanoate