MilliporeSigma™ Calbiochem™ WRN Helicase Inhibitor, NSC 19630

Description

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.

A cell-permeable maleimide compound selectively inhibits Werner syndrome WRN helicase activity (IC₅₀ = 20μM) over its ATPase and exonuclease activities (19% and <10% inhibition, respectively, at 50μM), 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 3μM 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 2μM treatment), enhanced DSB (17-fold increase in γ-H2AX foci staining after 72 h 2μM treatment), and increased S-phase population (from 24% to 42% after 72 h 2μM 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.

Specifications

• Color: White
• Description: 97% by NMR
• CAS: 72835-26-8
• Molecular Formula: C₈H₉NO₄
• Formula Weight: 183.2g/mol
• Solubility: DMSO or EtOH
• Form: Solid
• Quantity: 5 mg