681647
WRN Helicase Inhibitor, NSC 19630
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(s):
WRN Helicase Inhibitor, NSC 19630, 1-((1-Oxopropoxy)methyl)-maleimide, 1-((1-Oxopropoxy)methyl)-1H-pyrrole-2,5-dione, MIRA-1, p53 Activator VIII
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About This Item
Empirical Formula (Hill Notation):
C8H9NO4
CAS Number:
Molecular Weight:
183.16
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
assay
≥97% (NMR)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
white
solubility
DMSO: 50 mg/mL, ethanol: 50 mg/mL
shipped in
ambient
storage temp.
2-8°C
SMILES string
N1(C(=O)C=CC1=O)COC(=O)CC
InChI
1S/C8H9NO4/c1-2-8(12)13-5-9-6(10)3-4-7(9)11/h3-4H,2,5H2,1H3
InChI key
YXEWPGYLMHXLPS-UHFFFAOYSA-N
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.
Preparation Note
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.
Bykov, V.J.N., et al. 2005. J. Biol. Chem.280, 30384.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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