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

681647
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₈H₉NO₄ 72835-26-8

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      681647-5MG
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          Glass bottle 5 mg
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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 Image
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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 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.