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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

567860
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
925434-55-5C₂₅H₂₃N₇OS

Products

Catalogue NumberPackaging Qty/Pack
567860-10MG Glass bottle 10 mg
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
Catalogue 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.