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681647 Sigma-Aldrich

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

The WRN Helicase Inhibitor, NSC 19630, also referenced under CAS 72835-26-8, controls the biological activity of WRN Helicase. This small molecule/inhibitor is primarily used for Cell Signaling applications.

Synonym: 1-((1-Oxopropoxy)methyl)-maleimide, 1-((1-Oxopropoxy)methyl)-1H-pyrrole-2,5-dione, MIRA-1, p53 Activator VIII, WRN Helicase Inhibitor, NSC 19630 - CAS 72835-26-8 - Calbiochem

  • CAS Number 72835-26-8

  • Empirical Formula (Hill Notation) C8H9NO4

  • Molecular Weight 183.16

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Properties

Related Categories Cell Biology, Cell Signaling and Neuroscience, Cyclic Nucleotide Metabolism, G Proteins and Cyclic Nucleotides, Phosphodiesterase Inhibitors More...
Quality Level   100
assay   ≥97% (NMR)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
storage conditions   +2C to +8C
color   white
solubility   DMSO: 50 mg/mL
  ethanol: 50 mg/mL
shipped in   ambient

Description

General description

A 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.

Packaging

5 mg in Glass bottle

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Aggarwal, M., et al. 2011. Proc. Natl. Acad. Sci USA108, 1525.
Bykov, V.J.N., et al. 2005. J. Biol. Chem.280, 30384.

Safety & Documentation

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