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