444153
MDM2/MDMX Dual Inhibitor, RO-5963
别名:
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
方案
≥98% (HPLC)
质量水平
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
desiccated (hygroscopic)
protect from light
颜色
orange-brown
溶解性
DMSO: 100 mg/mL
运输
ambient
储存温度
−20°C
一般描述
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.
生化/生理作用
Cell permeable: yes
Primary Target
MDMX
MDMX
Reversible: yes
Secondary Target
MDM2
MDM2
包装
Packaged under inert gas
制备说明
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Graves, B., et al. 2012. Proc. Natl. Acad. Sci. USA109, 11788.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
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