1. PROTAC
  2. Ligands for E3 Ligase
  3. 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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MEL23 Chemical Structure

MEL23 Chemical Structure

CAS No. : 642072-49-9

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Description

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[1].

IC50 & Target[1]

MDM2

 

In Vitro

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.

Cell Viability Assay[1]

Cell Line: RKO cells
Concentration: 3.16-100 μM
Incubation Time: 48 hours
Result: Specifically decreased RKO cell viability.

Cell Cycle Analysis[1]

Cell Line: HT-1080 cells
Concentration: 2.5 μg/mL (7 μM), 5 μg/mL (14 μM)
Incubation Time: 48 hours
Result: Increased the sub-G1 population and caused a slight G2-cell cycle arrest.

Western Blot Analysis[1]

Cell Line: U2OS, RKO, and HCT116 cells (p53 wild-type)
Concentration: 5 μg/mL (14 μM)
Incubation Time: 6 hours
Result: Increased the Mdm2 and p53 levels.

RT-PCR[1]

Cell Line: RKO cells
Concentration: 5 μg/mL (14 μM)
Incubation Time: 24 hours, 48 hours
Result: Increased the transcription of p53 target genes, Mdm2, p21, puma, and bax.
Molecular Weight

354.40

Formula

C19H22N4O3

CAS No.
SMILES

O=C1NC(C(C2NCCC3=C2NC4=C3C=CC=C4)C(N1CCCC)=O)=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MEL23
Cat. No.:
HY-148106
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