MEL23
MEL23 is a MDM2 E3 ligase inhibitor that blocks the E3 ligase activity of the MDM2-MDMX complex. MEL23 inhibits Mdm2 and p53 ubiquitination in cells, reduce viability of cells with wild-type p53. MEL23 stabilizes MDM2 via a mechanism independent of p53 transcription.
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- CAS. Nr.: 642072-49-9
- Formel: C19H22N4O3
- Molecular Weight:354.40
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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MDM2 |
MEL23 increases the luminescence of Mdm2(wt)-luciferase cells with an EC50 value of 2.7 μg/mL[1].
MEL23 (3.16-100 μM; 48 hours) leads to cell death that is p53-dependent[1].
MEL23 (2.5-5 μg/mL; 48 hours) increases the sub-G1 population and caused a slight G2-cell cycle arrest in HT-1080 cells[1].
MEL23 (5 μg/mL; 6 hours) increases levels of Mdm2, p53, and MdmX and activates p53[1].
MEL23 (5 μg/mL; 24-48 hours) increases the transcription of p53 target genes, Mdm2, p21, puma, and bax[1].
In the parental HT-1080 cells, MEL23 suppresses cell death induced by Erastin (HY-15763), and substantially decreases the extent of ferroptosis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RKO cells
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Concentration:3.16-100 μM
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Incubation Time:48 hours
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Result:Specifically decreased RKO cell viability.
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Cell Line:HT-1080 cells
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Concentration:2.5 μg/mL (7 μM), 5 μg/mL (14 μM)
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Incubation Time:48 hours
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Result:Increased the sub-G1 population and caused a slight G2-cell cycle arrest.
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Cell Line:U2OS, RKO, and HCT116 cells (p53 wild-type)
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Concentration:5 μg/mL (14 μM)
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Incubation Time:6 hours
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Result:Increased the Mdm2 and p53 levels.
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Cell Line:RKO cells
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Concentration:5 μg/mL (14 μM)
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Incubation Time:24 hours, 48 hours
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Result:Increased the transcription of p53 target genes, Mdm2, p21, puma, and bax.
Chemical Information
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CAS. Nr. 642072-49-9
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Molecular Weight 354.40
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Formel C19H22N4O3
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SMILES
O=C1NC(C(C2NCCC3=C2NC4=C3C=CC=C4)C(N1CCCC)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Herman AG, et al. Discovery of Mdm2-MdmX E3 ligase inhibitors using a cell-based ubiquitination assay. Cancer Discov. 2011 Sep;1(4):312-25. [Content Brief]
[2]. Divya Venkatesh, et al. MDM2 and MDMX promote ferroptosis by PPARα-mediated lipid remodeling. Genes Dev. 2020 Apr 1;34(7-8):526-543. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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