Nicotinamide Phosphoribosyltransferase Inhibitor, FK866, 1 X 2 mg (481908-2MG)

A cell-permeable pyridinylacrylamide compound that acts as a selective, allosteric NAPRT/NAMPT (nicotinamide phosphoribosyltransferase) inhibitor (Kᵢ = 0.4 nM for the enzyme/substrate complex; Kᵢ′ = 0.3 nM for the free enzyme), while exhibiting no effect toward NPRT (nicotinic acid phosphoribosyltransferase) activity (82% inhibition of NAPRT activity at 10 nM vs no inhibition of NPRT activity at 1 µM in K-562 extract). FK866 treatment is shown to induce cell death by depleting NAD⁺ (Cat. Nos. 481911 & 481915) in HepG2 and NIH-3T3 cultures (by >95% after 24 h treatment of 10 nM FK866), likewise the addition of exogenous NAD⁺ is demonstrated to rescue NIH-3T3 and SH-SY5Y from FK866-induced NAD⁺-depletion and cell death. Supplied as a 50 mM (2 mg/102.17 µl) solution in DMSO. Formentini, L., et al. 2009. Biochem. Pharmacol.77, 1612. Nakahata, Y., et al. 2009. Science324, 654. Ramsey. K.M., et al. 2009. Science324, 651. Billington, R.A., et al. 2008. J. Biol. Chem.283, 6367. Hasmann, M. and Schemainda, I., 2003. Cancer Res.63, 7436. Toxicity: Standard Handling (A)

Read Less