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

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一般描述

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

包装

5 mg in Glass bottle

警告

Toxicity: Standard Handling (A)

重悬

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

其他说明

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

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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