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

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
72835-26-8C₈H₉NO₄

Products

Catalog NumberPackaging Qty/Pack
681647-5MG Glass bottle 5 mg
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
Global Trade Item Number
Catalog Number GTIN
681647-5MG 04055977260205

Documentation

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

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.