Atglistatin

Atglistatin is the first small molecule inhibitor of adipose triglyceride lipase (ATGL) – IC50 = 700 nM.1 It exhibits high selectivity for ATGL, is active in vitro and in vivo, and does not inhibit other key metabolic lipases. ATGL is the rate limiting enzyme in lipolysis and is thus an excellent target to reduce fatty acid mobilization and decrease lipotoxicity in metabolic syndrome. Inhibition of ATGL may be a useful strategy to attack the increased metabolic rate of cancerous cells.2