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530648 SIRT2 Inhibitor, AEM2 - Calbiochem

530648
  
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      Overview

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₂₇H₂₇N₃O
      Description
      Overview

      This product has been discontinued.



      A cell permeable methanophenanthridine derivative that acts a selective inhibitor of SIRT2 (IC50 = 3.8 µM) and exhibits ~30 fold greater selectivity over SIRT1 (IC50 > 100 µM) and SIRT3. Blocks SIRT2-induced p53 deacetylation and thereby elevates p53 levels and causes increased expression of CDKN1A, PUMA, and NOXA in non-small cell lung cancer (NSCLC) A549 cells. Also shown to reduce NSCLC cell viability by 50% (~20 µM) and inhibit their proliferation. Sensitizes A549 cancer cell line to etoposide (~1 µM) induced DNA damage in a p53-dependent manner.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.

      Catalogue Number530648
      Brand Family Calbiochem®
      SynonymsSirtuin 2 Inhibitor
      References
      ReferencesHoffmann G., et al. 2014. J. Biol. Chem. 289, 5208.
      Product Information
      FormWhite solid
      Hill FormulaC₂₇H₂₇N₃O
      Chemical formulaC₂₇H₂₇N₃O
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetSIRT2
      Primary Target IC<sub>50</sub>3.8 µM
      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 (-70°C). Stock solutions are stable for up to 1 month at -70°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      530648 0

      Documentation

      SIRT2 Inhibitor, AEM2 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Hoffmann G., et al. 2014. J. Biol. Chem. 289, 5208.
      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.

      Revision20-June-2014 JSW
      SynonymsSirtuin 2 Inhibitor
      DescriptionA cell permeable methanophenanthridine derivative that acts a selective inhibitor of SIRT2 (IC50 = 3.8 µM) and exhibits ~30 fold greater selectivity over SIRT1 (IC50 > 100 µM) and SIRT3. Blocks SIRT2-induced p53 deacetylation and thereby elevates p53 levels and causes increased expression of CDKN1A, PUMA, and NOXA in non-small cell lung cancer (NSCLC) A549 cells. Also shown to reduce NSCLC cell viability by 50% (~20 µM) and inhibit their proliferation. Sensitizes A549 cancer cell line to etoposide (~1 µM) induced DNA damage in a p53-dependent manner.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₇H₂₇N₃O
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 1 month at -70°C.
      Toxicity Standard Handling
      ReferencesHoffmann G., et al. 2014. J. Biol. Chem. 289, 5208.