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

481908
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₄H₂₉N₃O₂ 658084-64-1

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      481908-2MG
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          2 mg
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          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®
          Synonyms(E)-N-(4-(1-Benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide, NAMPT Inhibitor, NAPRT 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
          FormYellow liquid
          FormulationSupplied as a 50 mM (2 mg/102.17 µl) solution in DMSO.
          Hill FormulaC₂₄H₂₉N₃O₂
          Chemical formulaC₂₄H₂₉N₃O₂
          Structure formula ImageStructure formula Image
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          481908

          References

          Reference overview
          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.
          Data Sheet

          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.

          Revision11-April-2011 RFH
          Synonyms(E)-N-(4-(1-Benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide, NAMPT Inhibitor, NAPRT 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.
          FormYellow 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 +2°C to +8°C
          Protect from light
          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.