Description
Product Usage Information
BMS-303141 is supplied as a lyophilized powder. For a 15 mM stock, reconstitute 5 mg of powder in 0.79 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.
Storage
Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles .
Background
The small-molecule BMS-303141 is a potent (IC = 0.13 μM) inhibitor of ATP-citrate lyase (ACL). ACL catalyzes the formation of cytosolic acetyl-CoA and oxaloacetate (OAA) in the cytosol, which is the key step for fatty acid and cholesterol biosynthesis. BMS-303141 also weakly inhibits acetyl-CoA carboxylase (ACC) isoforms ACC1 and ACC2. Treatment of high-fat fed mice with BMS-303141 reduced weight gain and decreased levels of plasma cholesterol, triglycerides, and glucose (1). BMS-303141 treatment of prostate cancer cells impaired cell proliferation or induced death in androgen-depleted, castration-resistant prostate cancer cells (2). Hepatocellular carcinoma cells responded to treatment with BMS-303141, reducing cell proliferation and promoting apoptosis. BMS-303141 is thought to induce endoplasmic reticulum (ER) stress and activate the p-eIF2α/ATF4/CHOP pathway to promote apoptosis. The combined treatment of a mouse xenograft model with BMS-303141 and a protein kinase inhibitor reduced tumor volume and weight (3).
Alternate Names
3,5-Dichloro-2-hydroxy-N-(4-methoxy[1,1'-biphenyl]-3-yl)-benzenesulfonamide
