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567860 SRT1720 - CAS 925434-55-5 - Calbiochem

SRT1720, CAS 925434-55-5, is a cell-permeable inhibitor of the mitochondrial SIRT3. Inhibition is AceCS2-competitive (Ki = 0.56 µM; Km = 2.44 µM), but NAD+-uncompetitive (Ki = 0.34 µM; Km = 280 µM).

SRT1720 - CAS 925434-55-5 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N-(2-(3-(1-Piperazinylmethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)-2-quinolinecarboxamide, Sirtuin-3 Inhibitor, SRT1720, HAT Inhibitor XI, Histone Acetyltransferase Inhibitor XI, p300/CBP Inhibitor IX, SIRT3 Inhibitor II

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567860
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
925434-55-5C₂₅H₂₃N₇OS

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      Description
      OverviewA cell-permeable quinolinecarboxamide compound that is shown to inhibit the mitochondrial SIRT3 in a substrate AceCS2-competitive (Ki = 0.56 µM; Km = 2.44 µM), but NAD+-uncompetitive (Ki = 0.34 µM; Km = 280 µM), manner. Also reported to decrease cellular p53 Lys382 acetylation (Effective conc. = 10 µM in U2OS and MEF cultures) and inhibit p300 HAT activity (IC50 = 9 µM) in vitro, as well as offer therapeutic benefits in several murine and rodent type 2 diabetes models (100 mg/kg/dayl p.o.) in vivo. Whether and how SRT1720 activates SIRT1 activity remains uncertain. Also available as a 25 mM solution in DMSO (Cat. No. 530748).
      Catalogue Number567860
      Brand Family Calbiochem®
      SynonymsN-(2-(3-(1-Piperazinylmethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)-2-quinolinecarboxamide, Sirtuin-3 Inhibitor, SRT1720, HAT Inhibitor XI, Histone Acetyltransferase Inhibitor XI, p300/CBP Inhibitor IX, SIRT3 Inhibitor II
      References
      ReferencesBaur, J.A., et al. 2012. Nat. Rev. Drug Discov. 11, 443.
      Minor, R.K., et al. 2011. Sci. Rep. 1, 70.
      Huber, J.L., et al. 2010. Future Med. Chem. 2, 1751
      Pacholec, M., et al. 2010. J. Biol. Chem. 285, 8340
      Jin, L., et al. 2009. Protein Sci. 18, 514
      Feige, J.N., et al. 2008. Cell Metab. 8, 347
      Milne, J.C., et al. 2007. Nature 450, 712.
      Product Information
      CAS number925434-55-5
      FormYellow solid
      Hill FormulaC₂₅H₂₃N₇OS
      Chemical formulaC₂₅H₂₃N₇OS
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationSRT1720, CAS 925434-55-5, is a cell-permeable inhibitor of the mitochondrial SIRT3. Inhibition is AceCS2-competitive (Ki = 0.56 µM; Km = 2.44 µM), but NAD+-uncompetitive (Ki = 0.34 µM; Km = 280 µM).
      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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Regulatory Review
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalog Number GTIN
      567860-10MG 04055977190380

      Documentation

      SRT1720 - CAS 925434-55-5 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      SRT1720 - CAS 925434-55-5 - Calbiochem Certificates of Analysis

      TitleLot Number
      567860

      References

      Reference overview
      Baur, J.A., et al. 2012. Nat. Rev. Drug Discov. 11, 443.
      Minor, R.K., et al. 2011. Sci. Rep. 1, 70.
      Huber, J.L., et al. 2010. Future Med. Chem. 2, 1751
      Pacholec, M., et al. 2010. J. Biol. Chem. 285, 8340
      Jin, L., et al. 2009. Protein Sci. 18, 514
      Feige, J.N., et al. 2008. Cell Metab. 8, 347
      Milne, J.C., et al. 2007. Nature 450, 712.
      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.

      Revision02-October-2012 JSW
      SynonymsN-(2-(3-(1-Piperazinylmethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)-2-quinolinecarboxamide, Sirtuin-3 Inhibitor, SRT1720, HAT Inhibitor XI, Histone Acetyltransferase Inhibitor XI, p300/CBP Inhibitor IX, SIRT3 Inhibitor II
      DescriptionA cell-permeable quinolinecarboxamide compound that is shown to inhibit the mitochondrial SIRT3 in a substrate AceCS2- (Acetyl-CoA synthetase 2) competitive (Ki = 0.56 µM; Km = 2.44 µM; Vmax = 173.35 µM/min), but NAD+-uncompetitive (Ki = 0.34 µM; Km = 280 µM; Vmax = 0.86 µM/min), manner, indicative of NAD+ binding as a prerequisite for inhibitor binding. Also reported to decrease cellular p53 Lys382 acetylation (Effective conc. = 10 µM in U2OS and MEF cultures) and inhibit p300 HAT activity (IC50 = 9 µM) in vitro, as well as offer therapeutic benefits in several murine and rodent type 2 diabetes models (100 mg/kg/dayl p.o.) in vivo. Whether and how SRT1720 activates SIRT1 activity remains uncertain.
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number925434-55-5
      Chemical formulaC₂₅H₂₃N₇OS
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (2.5 mg/ml; clear, yellow solution)
      Storage Protect from light
      -20°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Regulatory Review
      ReferencesBaur, J.A., et al. 2012. Nat. Rev. Drug Discov. 11, 443.
      Minor, R.K., et al. 2011. Sci. Rep. 1, 70.
      Huber, J.L., et al. 2010. Future Med. Chem. 2, 1751
      Pacholec, M., et al. 2010. J. Biol. Chem. 285, 8340
      Jin, L., et al. 2009. Protein Sci. 18, 514
      Feige, J.N., et al. 2008. Cell Metab. 8, 347
      Milne, J.C., et al. 2007. Nature 450, 712.