Nicotinamide Phosphoribosyltransferase Inhibitor, FK866 – CAS 658084-64-1 – Calbiochem

Descrição detalhada : 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., 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.
Sinónimos : Nicotinamide Phosphoribosyltransferase Inhibitor, FK866 - CAS 658084-64-1 - Calbiochem; (E)-N-(4-(1-Benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide, NAMPT Inhibitor, APO866, NAMPTase Inhibitor I, PBEF Inhibitor I, Visfatin Inhibitor I, NAPRT Inhibitor; APO866, NAMPTase Inhibitor I, PBEF Inhibitor I, Visfatin Inhibitor I, NAPRT Inhibitor, (E)-N-(4-(1-Benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide, NAMPT Inhibitor
Fórmula molecula r: C24H29N3O2
Armazenamento : 2-8C; 2-8C; 2-8C
Embalagem : 1X2MG