Cerulenin
Fatty Acid Synthase inhibitor / Fatty acid synthase (FAS) inhibitor. Binds to β-keto-acyl-ACP synthase (KAS; IC50=1.5 μM), thus inhibiting protein acylation at concentrations of 45-134 μM1. Produces metabolic effects similar to the effects of leptin, but through mechanisms that are independent of, or down-stream of, both leptin and melanocortin receptors2. Reduces nutrient-induced insulin release from normal rat islets3. Induces apoptosis in human melanoma A-375 cells4.
Biochemicals & reagents
17397-89-6
1) Yasuno et al. (2004), Identification and molecular characterization of the beta-ketoacyl-[acyl carrier protein] synthase component of the Arabidopsis mitochondrial fatty acid synthase; J. Biol. Chem., 279 8242 2) Makimura et al. (2001), Cerulenin mimics effects of leptin on metabolic rate, food intake, and body weight independent of the melanocortin system, but unlike leptin, cerulenin fails to block neuroendocrine effects of fasting; Diabetes, 50 733 3) Metz et al. (1993), Modulation of insulin secretion from normal rat islets by inhibitors of the post-translational modifications of GTP-binding proteins; Biochem. J., 295 31 4) Ho et al. (2007), Fatty acid synthase inhibitors cerulenin and C75 retard growth and induce caspase-dependent apoptosis in human melanoma A-375 cells; Biomed. Phamacother., 61 578
-20°C
TARGET: Antibiotic; Acyltransferase -- PATHWAY: Fatty acid metabolism; Apoptosis inducer -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer; DiabetesInfectious disease