MDM2 E3 Ligase Inhibitor III, MEL23

MDM2 Inhibitor VII, MEL23
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.
产品信息
Form  Yellow solid
Molar mass  354.4
Protect from Light  是的
Packaged under inert gas  是的
Purity  ≥95% by HPLC
Solubility  DMSO
Chemical formula  C19H22N4O3
商店和运输信息
Storage  +2°C to +8°C
Ship  Ambient Temperature Only
Standard Handling