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373227 MDM2 Inhibitor VII, MEL23 - Calbiochem

373227
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₉H₂₂N₄O₃

Products

Catalogue NumberPackaging Qty/Pack
373227-10MG Glass bottle 10 mg
Description
OverviewA 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.
Catalogue Number373227
Brand Family Calbiochem®
Synonyms3-Butyl-6-hydroxy-5-(2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)pyrimidine-2,4(1H,3H)-dione, MDM2-MDMX E3 Ligase Inhibitor
References
ReferencesHerman, A.G., et al. 2011. Cancer Discovery 1, 312.
Product Information
FormYellow solid
Hill FormulaC₁₉H₂₂N₄O₃
Chemical formulaC₁₉H₂₂N₄O₃
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥95% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

MDM2 Inhibitor VII, MEL23 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

MDM2 Inhibitor VII, MEL23 - Calbiochem Certificates of Analysis

TitleLot Number
373227

References

Reference overview
Herman, A.G., et al. 2011. Cancer Discovery 1, 312.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision24-September-2012 JSW
Synonyms3-Butyl-6-hydroxy-5-(2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)pyrimidine-2,4(1H,3H)-dione, MDM2-MDMX E3 Ligase Inhibitor
DescriptionA 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.
FormYellow solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₉H₂₂N₄O₃
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (2.5 mg/ml; clear, pale yellow solution)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesHerman, A.G., et al. 2011. Cancer Discovery 1, 312.