Millipore Sigma Vibrant Logo
Attention: We have moved. Merck Millipore products are no longer available for purchase on MerckMillipore.com.Learn More

481908 Nicotinamide Phosphoribosyltransferase Inhibitor, FK866 - CAS 658084-64-1 - Calbiochem

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.

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: NAPRT Inhibitor, (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

481908
Purchase on Sigma-Aldrich

Aperçu

Replacement Information

Tableau de caractéristiques principal

CAS #Empirical Formula
658084-64-1C₂₄H₂₉N₃O₂

Products

RéférenceConditionnement Qté
481908-2MG 2 mg
Description
OverviewA 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.
Catalogue Number481908
Brand Family Calbiochem®
SynonymsNAPRT Inhibitor, (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
References
ReferencesFormentini, L., et al. 2009. Biochem. Pharmacol. 77, 1612.
Nakahata, Y., et al. 2009. Science 324, 654.
Ramsey. K.M., et al. 2009. Science 324, 651.
Billington, R.A., et al. 2008. J. Biol. Chem. 283, 6367.
Hasmann, M. and Schemainda, I., 2003. Cancer Res. 63, 7436.
Product Information
CAS number658084-64-1
FormColorless to yellow liquid
FormulationSupplied as a 50 mM (2 mg/102.17 µl) solution in DMSO.
Hill FormulaC₂₄H₂₉N₃O₂
Chemical formulaC₂₄H₂₉N₃O₂
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥97% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Référence GTIN
481908-2MG 04055977225532

Documentation

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

Titre

Fiche de données de sécurité des matériaux (FDS) 

Nicotinamide Phosphoribosyltransferase Inhibitor, FK866 - CAS 658084-64-1 - Calbiochem Certificats d'analyse

TitreNuméro de lot
481908

Références bibliographiques

Aperçu de la référence bibliographique
Formentini, L., et al. 2009. Biochem. Pharmacol. 77, 1612.
Nakahata, Y., et al. 2009. Science 324, 654.
Ramsey. K.M., et al. 2009. Science 324, 651.
Billington, R.A., et al. 2008. J. Biol. Chem. 283, 6367.
Hasmann, M. and Schemainda, I., 2003. Cancer Res. 63, 7436.
Fiche technique

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision06-May-2020 JSW
SynonymsNAPRT Inhibitor, (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
DescriptionA 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.
FormColorless to yellow liquid
FormulationSupplied as a 50 mM (2 mg/102.17 µl) solution in DMSO.
Intert gas (Yes/No) Packaged under inert gas
CAS number658084-64-1
Chemical formulaC₂₄H₂₉N₃O₂
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Toxicity Standard Handling
ReferencesFormentini, L., et al. 2009. Biochem. Pharmacol. 77, 1612.
Nakahata, Y., et al. 2009. Science 324, 654.
Ramsey. K.M., et al. 2009. Science 324, 651.
Billington, R.A., et al. 2008. J. Biol. Chem. 283, 6367.
Hasmann, M. and Schemainda, I., 2003. Cancer Res. 63, 7436.