373227

MDM2 Inhibitor VII, MEL23

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

• Synonym(e): MDM2 Inhibitor VII, MEL23, 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
• Empirische Formel (Hill-System): C₁₉H₂₂N₄O₃
• CAS-Nummer: 642072-49-9
• Molekulargewicht: 354.40
• MDL-Nummer: MFCD03662093
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥95% (HPLC)
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: yellow
• Löslichkeit: DMSO: 2.5 mg/mL, clear, pale yellow
• Versandbedingung: ambient
• Lagertemp.: 2-8°C
• SMILES String: OC1=C(C(N(CCCC)C(N1)=O)=O)C(NCC2)C3=C2C4=C(N3)C=CC=C4

Beschreibung

Allgemeine Beschreibung

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.

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 1
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable