481908

Nicotinamide Phosphoribosyltransferase Inhibitor, FK866

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.

• Sinónimos: Nicotinamide Phosphoribosyltransferase Inhibitor, FK866, (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 empírica (notación de Hill): C₂₄H₂₉N₃O₂
• Número de CAS: 658084-64-1
• Peso molecular: 391.51
• Número MDL: MFCD10565943
• Código UNSPSC: 51111800
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥97% (HPLC)
• Formulario: liquid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: yellow
• solubilidad: DMSO: 100 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 2-8°C
• cadena SMILES: N2(CCC(CC2)CCCCNC(=O)\C=C\c3cnccc3)C(=O)c1ccccc1
• InChI: 1S/C24H29N3O2/c28-23(12-11-21-8-6-15-25-19-21)26-16-5-4-7-20-13-17-27(18-14-20)24(29)22-9-2-1-3-10-22/h1-3,6,8-12,15,19-20H,4-5,7,13-14,16-18H2,(H,26,28)/b12-11+
• Clave InChI: KPBNHDGDUADAGP-VAWYXSNFSA-N

Descripción

Descripción general

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.

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Forma física

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

Otras notas

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.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 2
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable