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681647 WRN Helicase Inhibitor, NSC 19630 - CAS 72835-26-8 - Calbiochem

681647
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Empirical FormulaCAS #
C₈H₉NO₄ 72835-26-8

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681647-5MG
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      Description
      OverviewA cell-permeable maleimide compound selectively inhibits Werner syndrome WRN helicase activity (IC50 = 20 µM) over its ATPase and exonuclease activities (19% and <10% inhibition, respectively, at 50 µM), while exhibiting no effect against the helicase activity of two other human RecQ family DNA helicases (RECQ1 and Werner syndrome BLM), Fanconi anemia group J helicase FANCJ, as well as three other E. coli helicases, RecQ, UvrD, and DnaB. The WRN-dependent antiproliferation activity of MIRA-1/NSC 19630 in HeLa 1.2.11 cultures (0% vs. 95% inhibition with or without siRNA-mediated WRN-depletion, respectively, after 48 h 3 µM treatment) is shown to be a direct result of apoptosis induction due to replication forks blockage (20-fold increase in PCNA foci staining after 72 h 2 µM treatment), enhanced DSB (17-fold increase in γ-H2AX foci staining after 72 h 2 µM treatment), and increased S-phase population (from 24% to 42% after 72 h 2 µM treatment). In some cells, MIRA-1/NSC 19630 appears to also exert its apoptotic effect, at least in part, by restoring DNA-binding and transactivation function of some, but not all, p53 mutants.
      Catalogue Number681647
      Brand Family Calbiochem®
      Synonyms1-((1-Oxopropoxy)methyl)-maleimide, 1-((1-Oxopropoxy)methyl)-1H-pyrrole-2,5-dione, MIRA-1, p53 Activator VIII
      References
      ReferencesAggarwal, M., et al. 2011. Proc. Natl. Acad. Sci USA 108, 1525.
      Bykov, V.J.N., et al. 2005. J. Biol. Chem. 280, 30384.
      Product Information
      CAS number72835-26-8
      FormWhite solid
      Hill FormulaC₈H₉NO₄
      Chemical formulaC₈H₉NO₄
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥97% by NMR
      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 Standard Handling
      Storage +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 6 months at -20°C.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      WRN Helicase Inhibitor, NSC 19630 - CAS 72835-26-8 - Calbiochem MSDS

      Title

      Safety Data Sheet (SDS) 

      WRN Helicase Inhibitor, NSC 19630 - CAS 72835-26-8 - Calbiochem Certificates of Analysis

      TitleLot Number
      681647

      References

      Reference overview
      Aggarwal, M., et al. 2011. Proc. Natl. Acad. Sci USA 108, 1525.
      Bykov, V.J.N., et al. 2005. J. Biol. Chem. 280, 30384.
      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.

      Revision30-Sepmtember-2011 RFH
      Synonyms1-((1-Oxopropoxy)methyl)-maleimide, 1-((1-Oxopropoxy)methyl)-1H-pyrrole-2,5-dione, MIRA-1, p53 Activator VIII
      DescriptionA cell-permeable maleimide compound selectively inhibits Werner syndrome WRN helicase activity (IC50 = 20 µM) over its ATPase and exonuclease activities (19% and <10% inhibition, respectively, at 50 µM), while exhibiting no effect against the helicase activity of two other human RecQ family DNA helicases (RECQ1 and Werner syndrome BLM), Fanconi anemia group J helicase FANCJ, as well as three other E. coli helicases, RecQ, UvrD, and DnaB. The WRN-dependent antiproliferation activity of MIRA-1/NSC 19630 in HeLa 1.2.11 cultures (0% vs. 95% inhibition with or without siRNA-mediated WRN-depletion, respectively, after 48 h 3 µM treatment) is shown to be a direct result of apoptosis induction due to replication forks blockage (20-fold increase in PCNA foci staining after 72 h 2 µM treatment), enhanced DSB (17-fold increase in γ-H2AX foci staining after 72 h 2 µM treatment), and increased S-phase population (from 24% to 42% after 72 h 2 µM treatment). In some cells, MIRA-1/NSC 19630 appears to also exert its apoptotic effect, at least in part, by restoring DNA-binding and transactivation function of some, but not all, p53 mutants.
      FormWhite solid
      CAS number72835-26-8
      Chemical formulaC₈H₉NO₄
      Structure formulaStructure formula
      Purity≥97% by NMR
      SolubilityDMSO (50 mg/ml) or Ethanol (50 mg/ml)
      Storage +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 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesAggarwal, M., et al. 2011. Proc. Natl. Acad. Sci USA 108, 1525.
      Bykov, V.J.N., et al. 2005. J. Biol. Chem. 280, 30384.