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373227 Sigma-Aldrich

MDM2 Inhibitor VII, MEL23 - Calbiochem

The MDM2 Inhibitor VII controls the biological activity of MDM2. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

Synonym: MDM2 Inhibitor VII, MEL23 - Calbiochem, MDM2-MDMX E3 Ligase Inhibitor, 3-Butyl-6-hydroxy-5-(2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)pyrimidine-2,4(1H,3H)-dione

  • Empirical Formula (Hill Notation) C19H22N4O3

  • Molecular Weight 354.40

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Properties

Related Categories Molecular Biology, Post-Translational Modification, Proteomics, Ubiquitination Analysis
Quality Level   100
assay   ≥95% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   +2C to +8C
color   yellow
solubility   DMSO: 2.5 mg/mL, clear, pale yellow
shipped in   ambient

Description

General description

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.

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.

Packaging

10 mg in Glass bottle

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Safety & Documentation

Safety Information

WGK Germany 
WGK 1
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable
Protocols & Articles
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