Application

Fasnall benzenesulfonate salt has been used as a fatty acid synthase inhibitor to test its effect on hypoxic U87 MG cells in cell viability assay and lipid droplet formation assay.

Biochem/physiol Actions

Fasnall is a fatty acid synthase (FASN or FAS) inhibitor (IC₅₀ = 3.71 ?M by cell-free assay with 200 µM NADPH; IC₅₀ = 147 and 213 nM against acetate and glucose lipids incorporation in HepG2 cells) composed of two enantiomers (HS-79 and HS-80) that selectively target FASN co-factor nucleotide-binding sites without affecting ACC, ZipK, AMPKα, AMPKγ, TRAP1, HSP70, NS5, IRAK2 nucleotide binding or the ATP-binding activity of BT474 cellular proteins. Fasnall is shown to completely block the proliferation in multiple breast cancer cultures at 50 µM as a result of apoptosis induction with much reduced cytotoxicity than C75 toward the non-tumorigenic cell line MCF10A. When administered via i.p. injection, Fasnall is efficacious in prolonging the survival of MMTV-Neu mice by effectively suppressing mammary adenocarcinoma tumor progression (15 mg/kg dosed alone twice weekly or 50 mg/kg dosed with carboplatin once weekly).