FK-866, 5 mg

Offered by STEMCELL Technologies as a small molecule research reagent, this compound is a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), the enzyme that regulates NAD+ biosynthesis from the natural precursor nicotinamide. In hepatocarcinoma cells, the inhibitor activates AMP-activated protein kinase (AMPK) and downregulates mammalian target of rapamycin (mTOR) signaling.

The reagent is supplied as a crystalline solid with a stated purity of >= 98% and a CAS number of 658084-64-1. Its chemical name is N-[4-(1-benzoyl-4-piperidinyl)butyl]-3-(3-pyridinyl)-2E-propenamide, with chemical formula C24H29N3O2. The product is stable at -20C as supplied for 12 months from date of receipt, and should be protected from prolonged exposure to light; long-term storage with a desiccant is recommended. Reported solubility values are PBS <= 1.2 mM, DMSO <= 60 mM, and absolute ethanol <= 100 mM.

Published applications include use in metabolism research to deplete NAD+ and in cancer research. In HepG2 human liver carcinoma cells, the compound induces delayed cell death by apoptosis with an IC50 of ~1 nM, and it triggers autophagic death in SH-SY5Y neuroblastoma cells with an IC50 of 0.93 nM. Dose-dependent cytotoxicity has been reported in multiple myeloma cells. For use as a cell culture supplement, stock solution should be diluted into culture medium immediately before use, with final DMSO concentration kept at or below 0.1% to avoid potential cell toxicity.