MilliporeSigma™ Calbiochem™ Nicotinamide Phosphoribosyltransferase Inhibitor, FK866

Description

The Nicotinamide Phosphoribosyltransferase Inhibitor, FK866, also referenced under CAS 658084-64-1, controls the biological activity of Nicotinamide Phosphoribosyltransferase. This small molecule/inhibitor is primarily used for Neuroscience applications.

A cell-permeable pyridinylacrylamide compound that acts as a selective, allosteric NAPRT/NAMPT (nicotinamide phosphoribosyltransferase) inhibitor (K_i = 0.4nM for the enzyme/substrate complex; K_i^′ = 0.3nM for the free enzyme), while exhibiting no effect toward NPRT (nicotinic acid phosphoribosyltransferase) activity (82% inhibition of NAPRT activity at 10nM vs no inhibition of NPRT activity at 1μM in K-562 extract). FK866 treatment is shown to induce cell death by depleting NAD⁺ (Cat. Nos. 481911 and 481915) in HepG2 and NIH-3T3 cultures (by >95% after 24 h treatment of 10nM FK866), likewise the addition of exogenous NAD⁺ is demonstrated to rescue NIH-3T3 and SH-SY5Y from FK866-induced NAD⁺-depletion and cell death.

Specifications

• Color: Yellow
• Formulation: Supplied as a 50 mM (2mg/102.17μl) solution in DMSO.
• Description: 97% by HPLC
• CAS: 658084-64-1
• Molecular Formula: C₂₄H₂₉N₃O₂
• Formula Weight: 391.5g/mol
• Solubility: DMSO
• Content And Storage: Protect from light
• Form: Liquid
• Quantity: 2 mg