Acetyl-CoA carboxylase catalyzes the ATP-dependent carboxylation of acetyl-CoA, a rate-limiting step in fatty acid biosynthesis.Acetyl-CoA carboxylase is a desirable target for the development of drugs to treat diabetes, cancer, and other diseases because of its critical roles in fatty acid metabolism.
Animals have two main ACC isoforms, ACC1 and ACC2, which are each encoded by a different gene and have different distributions in different tissues and cells. ACC, which is mediated by the related enzymes ACC1 and ACC2, catalyzes the ATP-dependent carboxylation of acetyl-CoA to form malonyl-CoA as the first committed step of fatty acid synthesis (FASyn). While ACC2 is attached to the mitochondrial outer membrane, where localized malonyl-CoA production inhibits carnitine palmitoyltransferase-1 (CPT-1) function to stop fatty acids from entering the mitochondria to undergo fatty acid oxidation (FAOxn), ACC1 encodes a cytoplasmic isoform that is thought to be the predominant isoform controlling FASyn.
|CP-640186 is a novel, potent and and cell-permeableinhibitor of mammalian ACCs (isozyme-nonselective acetyl-CoA carboxylase) with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively; It hash improved metabolic stability in comparison to CP-610431, an analog of CP-640186.
|Firsocostat (formerly also known as ND-630; GS-0976; NDI-010976; ND630) is a novel and potent inhibitor of ACC (acetyl-CoA carboxylase) with IC50 values of 2.1 and 6.1 nM for human ACC1 and ACC2, respectively.
|ND-646 is-an allosteric inhibitor of the ACC enzymes ACC1 and ACC2 that prevents ACC subunit dimerization-to suppress fatty acid synthesis in vitro and in vivo.
|PF-05175157 (PF05175157) is a novel, potent and selective broad spectruminhibitor of acetyl-CoA carboxylase(ACC) with anti-diabetic and anticancer activity.
|TOFA (5‑tetradecyloxy‑2‑furoic acid), also known as RMI14514 and MDL14514, is an allosteric inhibitor of acetyl-CoA carboxylase-α (ACCA).