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566332 Sirt1 Inhibitor VII, Inauhzin - Calbiochem

The Sirt1 Inhibitor VII, Inauhzin controls the biological activity of Sirt1. This small molecule/inhibitor is primarily used for Cell Structure applications.

Sirt1 Inhibitor VII, Inauhzin - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 10-[2-(5H-[1,2,4]triazino[5,6-b]indol-3-ylthio)butanoyl]-10H-phenothiazine, INZ

Primary Target: Sirt1
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566332
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₅H₁₉N₅OS₂

Pricing & Availability

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      Description
      OverviewA cell-permeable phenothiazine derivative that selectively inhibits SirT1 (IC50 ≤2.0 µM), but not SirT2, SirT3, or HCAC8 (IC50 >50 µM), activity. Effectively elevates cellular p53 lysine acetylation (Effective conc. 2 µM), thereby protecting p53 lysine residues from MDM2-mediated ubiquitination without inhibiting MDM2 activity toward deacetylated p53. Shown to inhibit cancer cell growth in a p53-dependent manner (IC50 = 2.0 and 15.7µM, respectively, against HCT116p53+/+ and HCT116p53-/- cells) and synergize with Nutlin-3 (Cat. Nos. 444143, 444151, & 444152) in blocking HCT116p53+/+ proliferation in vitro (1 µM INZ & 4 µM Nutlin-3) and inducing HCT116p53+/+ apoptosis in mice in vivo (15 mg INZ/kg/d i.p; 150 mg Nut-3/kg/12 h p.o.).
      Catalogue Number566332
      Brand Family Calbiochem®
      Synonyms10-[2-(5H-[1,2,4]triazino[5,6-b]indol-3-ylthio)butanoyl]-10H-phenothiazine, INZ
      References
      ReferencesZhang, Q., et al. 2012. EMBO Mol. Med. 4, 298.
      Zhang, Y., et al. 2012. Cancer Biol. Ther. 13, 915
      Product Information
      FormBeige powder
      Hill FormulaC₂₅H₁₉N₅OS₂
      Chemical formulaC₂₅H₁₉N₅OS₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetSirt1
      Primary Target IC<sub>50</sub>0.7&ndash
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      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 Standard Handling
      Storage +2°C to +8°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
      566332-10MG 04055977191486

      Documentation

      Sirt1 Inhibitor VII, Inauhzin - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Sirt1 Inhibitor VII, Inauhzin - Calbiochem Certificates of Analysis

      TitleLot Number
      566332

      References

      Reference overview
      Zhang, Q., et al. 2012. EMBO Mol. Med. 4, 298.
      Zhang, Y., et al. 2012. Cancer Biol. Ther. 13, 915
      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-January-2013 JSW
      Synonyms10-[2-(5H-[1,2,4]triazino[5,6-b]indol-3-ylthio)butanoyl]-10H-phenothiazine, INZ
      DescriptionA cell-permeable phenothiazine derivative that selectively inhibits SirT1 (IC50 ≤2.0 µM), but not SirT2, SirT3, or HCAC8 (IC50 >50 µM), activity and effectively elevates cellular p53 lysine acetylation (Effective conc. 2 µM), thereby protecting p53 lysine residues from MDM2-mediated ubiquitination without directly inhibiting MDM2 function per se or its activity toward deacetylated p53. Shown to inhibit cancer cell growth in a p53-dependent manner (IC50 = 2.0 and 15.7µM, respectively, against HCT116p53+/+ and HCT116p53-/- cells) and synergize with Nutlin-3 (Cat. Nos. 444143, 444151, & 444152) in blocking HCT116p53+/+ proliferation in vitro (by 29%, 76%, and >98, respectively, with 1 µM INZ alone, 4 µM Nutlin-3 alone, or in combination) and inducing HCT116p53+/+ apoptosis in mice in vivo (3.5% above control TUNEL staining with either drug treatment alone or 25% with combined treatment; 15 mg INZ/kg via daily i.p; 150 mg Nut-3/kg b.i.d. p.o.).
      FormBeige powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₅H₁₉N₅OS₂
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°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 Standard Handling
      ReferencesZhang, Q., et al. 2012. EMBO Mol. Med. 4, 298.
      Zhang, Y., et al. 2012. Cancer Biol. Ther. 13, 915