A number of tumor cells and cell lines have been observed to have highly upregulated expression and activity of fatty acid synthase (FAS). Inhibition of FAS by the irreversible inhibitor cerulenin leads to cytotoxicity and apoptosis in human cancer cell lines,1 an effect believed to be mediated by the accumulation of malonyl-coenzyme A in cells with an upregulated FAS pathway.2 Cerulenin also leads to profound weight loss and feeding inhibition in both high-fat diet wild type obese and leptin-deficient ob/ob mice.3
1
Moche, M., Schneider, G., Edwards, P., et al. Structure of the complex between the antibiotic cerulenin and its target, β-ketoacyl-acyl carrier protein synthase. J Biol Chem274(10)6031-6034(1999).
2
Pizer, E.S., Thupari, J., Han, W.F., et al. Malonyl-coenzyme-A is a potential mediator of cytotoxicity induced by fatty-acid synthase inhibition in human breast cancer cells and xenografts. Cancer Res60213-218(2000).
3
Loftus, T.M., Jaworsky, D.E., Frehywot, G.L., et al. Reduced food intake and body weight in mice treated with fatty acid synthase inhibitors. Science2882379-2381(2000).
Formal Name
2R,3S-epoxy-4-oxo-7,10-dodecadienamide
CAS Number
17397-89-6
Molecular Formula
C12H17NO3
Formula Weight
223.3
Formulation
A crystalline solid
Purity
≥98%
Stability
2 years
Storage
-20°C
Shipping
Room temperature
in continental US; may vary elsewhere
SMILES
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C/C=C/C/C=C/CCC([C@@H]1[C@H](C(N)=O)O1)=O
Background Reading
Pizer, E.S., Thupari, J., Han, W.F., et al. Malonyl-coenzyme-A is a potential mediator of cytotoxicity induced by fatty-acid synthase inhibition in human breast cancer cells and xenografts. Cancer Res60213-218(2000).
Moche, M., Schneider, G., Edwards, P., et al. Structure of the complex between the antibiotic cerulenin and its target, β-ketoacyl-acyl carrier protein synthase. J Biol Chem274(10)6031-6034(1999).
Loftus, T.M., Jaworsky, D.E., Frehywot, G.L., et al. Reduced food intake and body weight in mice treated with fatty acid synthase inhibitors. Science2882379-2381(2000).
Cerulenin is available in the following screening
library: