CP-640186

CP-640186 is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 can also stimulate muscle fatty acid oxidation[1][2].

[1]Harwood HJ Jr, et al. Isozyme-nonselective N-substituted bipiperidylcarboxamide acetyl-CoA carboxylase inhibitors reduce tissue malonyl-CoA concentrations, inhibit fatty acid synthesis, and increase fatty acid oxidation in cultured cells and in experimental animals. J Biol Chem. 2003 Sep 26;278(39):37099-111.|[2]Yamashita T, et al. Design, synthesis, and structure-activity relationships of spirolactones bearing 2-ureidobenzothiophene as acetyl-CoA carboxylases inhibitors. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6314-8.|[3]Daniel Hess, et al. Inhibition of stearoylCoA desaturase activity blocks cell cycle progression and induces programmed cell death in lung cancer cells. PLoS One. 2010 Jun 30;5(6):e11394.Am J Transl Res. 2019 Nov 15;11(11):7104-7114.|bioRxiv. 2024 May 25.|Department of Microbiology & Immunology. Seoul National University Graduate School. 2015 Aug. |Front Oncol. 2021 Apr 22;11:665763.|Front Oncol. 2021 Apr 6.|Nat Commun. 2024 Oct 21;15(1):9062.|Nutrients. 2021 May 21;13(6):1740.|Viruses. 2019 Dec 10;11(12):1145.|J Exp Med. 2021 Dec 6;218(12):e20210639.