BMS-303141

BMS-303141 is a potent and cell-permeable small molecule inhibitor of ATP-citrate lyase (ACLY), with an IC50 of 0.13 μM. ACLY is a key metabolic enzyme that catalyzes the cytoplasmic conversion of citrate to acetyl-CoA, providing the essential building blocks for de novo fatty acid and cholesterol biosynthesis, as well as the acetyl groups required for histone acetylation. Developed by Bristol Myers Squibb, BMS-303141 has demonstrated therapeutic potential in preclinical models for metabolic disorders, including dyslipidemia, obesity, and type 2 diabetes, where it has been shown to reduce plasma triglycerides, cholesterol, and glucose levels. In the field of oncology, the compound is used to study the metabolic dependencies of various malignancies; research indicates it can inhibit cell proliferation in prostate cancer and hepatocellular carcinoma (HCC) and may help overcome resistance to tyrosine kinase inhibitors like lenvatinib. Although it is orally bioavailable and demonstrates significant pharmacological activity in vivo, BMS-303141 is currently utilized strictly as a research tool and has not been approved for clinical use.

Other names

3,5-dichloro-2-hydroxy-N-(4-methoxy[1,1'-biphenyl]-3-yl)-benzenesulfonamideCAS 943962-47-8CAS943962-47-8CAS-943962-47-8