atglistatin

Atglistatin is a selective and competitive small-molecule inhibitor of adipose triglyceride lipase (ATGL), also known as PNPLA2. ATGL is the rate-limiting enzyme in the lipolytic cascade, responsible for the hydrolysis of triglycerides into diglycerides and free fatty acids. By inhibiting ATGL with an IC50 of approximately 0.7 μM, atglistatin reduces the mobilization of fatty acids from cellular lipid droplets. Preclinical research has investigated atglistatin for its potential to treat metabolic disorders, including insulin resistance, type 2 diabetes, and hepatosteatosis, as well as its role in preventing cardiac dysfunction in heart failure. Additionally, recent studies suggest that atglistatin can sensitize acute myeloid leukemia (AML) cells to FLT3 inhibitors like gilteritinib by modulating lipid metabolism and ferroptosis. It is currently utilized as a research tool and has not been approved for clinical use in humans.

Other names

CAS 1469924-27-3CAS1469924-27-3CAS-1469924-27-3