444153

MDM2/MDMX Dual Inhibitor, RO-5963

• 別名: MDM2/MDMX Dual Inhibitor, RO-5963, MDM2 Inhibitor VIII, MDMX Inhibitor III, ( Z)-2-(4-((6-Chloro-7-methyl-1H-indol-3-yl)methylene)-2,5-dioxoimidazolidin-1-yl)-2-(3,4-difluorophenyl)-N-(1,3-dihydroxypropan-2-yl)acetamide, MDM2 Antagonist V, MDM2 Inhibitor VIII, MDMX Inhibitor III, (Z)-2-(4-((6-Chloro-7-methyl-1H-indol-3-yl)methylene)-2,5-dioxoimidazolidin-1-yl)-2-(3,4-difluorophenyl)-N-(1,3-dihydroxypropan-2-yl)acetamide, MDM2 Antagonist V
• 実験式（ヒル表記法）: C₂₄H₂₁ClF₂N₄O₅
• 分子量: 518.90
• UNSPSCコード: 12352200

特性

• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated (hygroscopic); protect from light
• 色: orange-brown
• 溶解性: DMSO: 100 mg/mL
• 輸送温度: ambient
• 保管温度: −20°C

詳細

詳細

A cell-permeable indolyl-hydantoin compound that simultaneously inhibits the interaction of both, MDM2 and MDMX with p53 (IC₅₀ = 17.3 and 24.7 nM, respectively, in vitro). Releases p53 from MDMX inhibition, stabilizes it, and fully restores its function. Shown to be far more superior to Nutlin-3a (>Cat. No. 444152) in blocking p53 interaction with MDMX. Binds to Phe, Trp, and Leu sub-pockets on the surface of MDMX and MDM2, and promotes MDMX and MDM2 dimer formation. Shown to induce cell cycle arrest in G1 and G2 phases. Also reported to induce apoptosis in several tumor cell lines expressing wild-type p53/MDMX (~ 10 to 20 µM). Its actions are not believed to be due to any genotoxic stress.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
MDMX

Reversible: yes

Secondary Target
MDM2

包装

Packaged under inert gas

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

Graves, B., et al. 2012. Proc. Natl. Acad. Sci. USA109, 11788.

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 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable