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.

• 別名: WRN Helicase Inhibitor, NSC 19630, 1-((1-Oxopropoxy)methyl)-maleimide, 1-((1-Oxopropoxy)methyl)-1H-pyrrole-2,5-dione, MIRA-1, p53 Activator VIII
• 実験式（ヒル表記法）: C₈H₉NO₄
• CAS番号: 72835-26-8
• 分子量: 183.16
• MDL番号: MFCD12828765
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥97% (NMR)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze
• 色: white
• 溶解性: DMSO: 50 mg/mL; ethanol: 50 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• SMILES記法: 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

詳細

詳細

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.

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 2
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable