Stemcell, 100-0264, FK-866

FK-866 is a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), an enzyme that regulates NAD+ biosynthesis from the natural precursor nicotinamide (Cameron et al.; Hasmann & Schemainda). In hepatocarcinoma cells, FK-866 activates AMP-activated protein kinase (AMPK) and downregulates mammalian target of rapamycin (mTOR) signaling (Schuster et al.).

METABOLISM

· FK-866 can be used to deplete NAD+, a central metabolism cofactor (Cameron et al.; Hasmann & Schemainda; Jadeja et al.).

CANCER RESEARCH

· Depletes NAD+ and induces delayed cell death by apoptosis in HepG2 human liver carcinoma cells (IC₅₀ = ~1 nM; Hasmann & Schemainda).

· Triggers dose-dependent cytotoxicity in multiple myeloma cells (Cea et al.).

· Induces autophagic death in neuroblastoma SH-SY5Y cells (IC₅₀ = 0.93 nM; Billington et al.).