MG Nicotinamide Phosphoribosylt 1PC x 2M

General description

A cell-permeable pyridinylacrylamide compound that acts as a selective, allosteric NAPRT/NAMPT (nicotinamide phosphoribosyltransferase) inhibitor (K_i = 0.4 nM for the enzyme/substrate complex; K_i^′ = 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.

A cell-permeable pyridinylacrylamide compound that acts as a selective, allosteric NAPRT/NAMPT (nicotinamide phosphoribosyltransferase) inhibitor (K_i = 0.4 nM for the enzyme/substrate complex; K_i^′ = 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

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.

Packaging

Packaged under inert gas

Physical form

Supplied as a 50 mM (2 mg/102.17 µl) solution in DMSO.

Warning

Toxicity: Standard Handling (A)