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MDM2 Inhibitor VII, MEL23-Calbiochem

品牌
Sigma-Aldrich
货号
373227
规格纯度
The MDM2 Inhibitor VII controls the biological activity of MDM2. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.
参考价格
3056.54 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

一般描述

A cell-permeable tetrahydro-β-carbolinylbarbiturate compound that selectively inhibits the E3 ligase activity of Mdm2-MdmX hetero-complex over that of Mdm2-Mdm2 homo-complex (70.6% vs. 17.6% inhibition, respectively, with 100 µM inhibitor), without affecting Mdm2-MdmX complex formation or the activity of Roc1-Cul1 and BRCA1-BARD1, two other ligase complexes that also utilize UbcH5C as the Ub-conjugating enzyme. Effectively inhibits Mdm2-MdmX E3 ligase activity-dependent ubiquitination and proteasomal degradation of cellular Mdm2 and p53 (effective conc. = 14 µM in U2OS, RKO, and HCT116 cultures) and prevents DNA damage-induced MdmX degradation in MCF7 cells upon 50 µM etoposide treatment. Shown to induce RKO and MEF cell death in a p53- and Mdm2-dependent manner. Unlike Nutlin-3 (Cat. Nos. 444143 & 444151), MEL23 does not act by interfering Mdm2-p53 interaction.
A cell-permeable tetrahydro-β-carbolinylbarbiturate compound that selectively inhibits the E3 ligase activity of Mdm2-MdmX hetero-complex over that of Mdm2-Mdm2 homo-complex (70.6% vs. 17.6% inhibition, respectively, at 100 µM), without affecting Mdm2-MdmX complex formation or the activity of two other UbcH5C-utilizing ligase complexes Roc1-Cul1 and BRCA1-BARD1. Effectively inhibits ubiquitination and proteasomal degradation of cellular Mdm2 and p53 (effective conc. = 14 µM in U2OS, RKO, and HCT116 cultures) and induce RKO and MEF cell death in a p53- and Mdm2-dependent manner. Unlike Nutlin-3 (Cat. Nos. 444143 & 444151), MEL23 does not interfere with Mdm2-p53 interaction.

包装

10 mg in Glass bottle
Packaged under inert gas

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

Herman, A.G., et al. 2011. Cancer Discovery1, 312.

法律信息

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

基本信息

经验(实验)分子式C19H22N4O3
分子量354.40
MDL编号MFCD03662093

产品性质

质量水平100
测定≥95% (HPLC)
形式solid
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 yellow
溶解性DMSO: 2.5 mg/mL, clear, pale yellow
运输ambient
储存温度2-8℃
SMILES stringOC1=C(C(N(CCCC)C(N1)=O)=O)C(NCC2)C3=C2C4=C(N3)C=CC=C4

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 1
闪点(F)Not applicable
闪点(C)Not applicable

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