Description
BMS-303141 (943963-47-8) is a potent and selective ATP citrate lyase (ACL) inhibitor, IC50=0.13 μM. Inhibits lipid biosynthesis, IC50=8 μM in HepG2 cells.1,2?Reduces weight gain, lowers plasma cholesterol, triglycerides and glucose in high-fat-fed mice.2?A novel tool compound for exploring the potential of ACL inhibition as a target for metabolic disorders such as obesity and dyslipidemia.2?Impairs proliferation or induces death in androgen-depleted castration resistant prostate cancer cells.3?Reduces cell cycle progression in iBN cells.4
Uses
BMS-303141 has been used for inhibition of ATP citrate lyase in breast cancer cell lines.
Definition
ChEBI: 3,5-dichloro-2-hydroxy-N-(2-methoxy-5-phenylphenyl)benzenesulfonamide is a member of biphenyls.
Biochem/physiol Actions
BMS-303141 is a potent inhibitor of ATP citrate lyase (ACL). BMS-303141 inhibits lipid synthesis in HepG2 cells with an IC50 of 8 μM, and lowers plasma triglycerides in a murine hyperlipdemia model.
References
1) Li?et al. (2007),?2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors; Bioorg. Med. Chem.,?17?3208
2) Ma?et al.?(2009),?A novel direct homogeneous assay for ATP citrate lyase; J. Lipid Res.,?50?2131
3) Shah?et al.?(2016),?Targeting ACLY sensitizes castration-resistant prostate cancer cells to AR antagonism by impinging on an ACLY-AMPK-AR feedback mechanism; Oncotarget,?7?43713
4) Rhee and Dekoter (2017),?Regulation of Lipid Metabolism and Cell Cycle Progression by PU.1 in Myeloid Progenitor Cells; Blood,?130?2433
