2. Apoptosis
  3. MDM-2/p53 Apoptosis
  4. MDMX/MDM2-IN-2

MDMX/MDM2-IN-2 is a potent p53-MDM2/MDMX dual inhibitors with Kis of 0.23 μM and 2.45 μM for MDM2 and MDMX, respectively. MDMX/MDM2-IN-2 inhibits the binding of p53 and MDM2 proteins. MDMX/MDM2-IN-2 restores the function of p53 and enables cell cycle arrest and apoptosis. MDMX/MDM2-IN-2 inhibits cell migration and invasion. MDMX/MDM2-IN-2 has antitumor activity.

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MDMX/MDM2-IN-2 Chemical Structure

MDMX/MDM2-IN-2 Chemical Structure

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MDMX/MDM2-IN-2 Related Antibodies

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Description

MDMX/MDM2-IN-2 is a potent p53-MDM2/MDMX dual inhibitors with Kis of 0.23 μM and 2.45 μM for MDM2 and MDMX, respectively. MDMX/MDM2-IN-2 inhibits the binding of p53 and MDM2 proteins. MDMX/MDM2-IN-2 restores the function of p53 and enables cell cycle arrest and apoptosis. MDMX/MDM2-IN-2 inhibits cell migration and invasion. MDMX/MDM2-IN-2 has antitumor activity[1].

IC50 & Target

Ki: 0.23 μM (MDM2) and 2.45 μM (MDMX)[1]
In Vitro

MDMX/MDM2-IN-2 demonstrates moderate anti-proliferative activities against HCT116 and SH-SY5Y cells (IC50=0.68 μM and 0.54 μM, respectively). MDMX/MDM2-IN-2 possesses low cytotoxicity on normal human lung epithelial BEAS-2B cells and LO2 liver cells (IC50=17.96 μM and 15.93 μM, respectively)[1].
MDMX/MDM2-IN-2 (0.6-2.4 μM; 48 h) induces apoptosis of HCT116 and SH-SY5Y cells[1].
MDMX/MDM2-IN-2 (0.6-2.4 μM; 48 h) arrests the cell cycle in G1 phase[1].
MDMX/MDM2-IN-2 (0.6-2.4 μM; 48 h) increases the levels of p53 and its downstream targets, MDM2, MDMX, p21 and cleaved-caspase3[1].
MDMX/MDM2-IN-2 (0.4-0.8 μM) dramatically inhibits colony formation, migration and invasion of HCT116 and SH-SY5Y cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MDMX/MDM2-IN-2 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HCT116 and SH-SY5Y cells
Concentration: 0.6, 1.2, 2.4 μM
Incubation Time: 48 h
Result: The percentages of apoptotic HCT116 and SH-SY5Y cells were 13.63% and 15.69% with 0.6 μM.
The percentage of apoptotic cells correspondingly increased to 37.6% and 40.8% with 2.4 μM.

Cell Cycle Analysis[1]

Cell Line: HCT116 and SH-SY5Y cells
Concentration: 0.6, 1.2, 2.4 μM
Incubation Time: 48 h
Result: There was an increase in the percentage of cancer cells at the G1 phase. Meanwhile, the percentage of G2 phase cells was relatively decreased.

Western Blot Analysis[1]

Cell Line: HCT116 and SH-SY5Y cells
Concentration: 0.6, 1.2, 2.4 μM
Incubation Time: 48 h
Result: Increased the levels of p53 and its downstream targets, MDM2, MDMX, p21 and cleaved-caspase3.

Cell Migration Assay [1]

Cell Line: HCT116 and SH-SY5Y cells
Concentration: 0.4, 0.6, 0.8 μM
Incubation Time: 48 h
Result: Significantly inhibited the migration and invasion in a dose-dependent manner.
Molecular Weight

576.87

Formula

C28H25Cl3FN3O3
SMILES

O=C(C(N(C1=CC=C(C=C1)Cl)C(CCC(N2CCNCC2)=O)=O)C3=CC=C(C=C3Cl)F)C4=CC=C(C=C4)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MDMX/MDM2-IN-2 Related Classifications

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Help & FAQs
  • 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.

Keywords:

MDMX/MDM2-IN-2MDM-2/p53Apoptosisp53MDMXmigrationinvasionantitumorG1 phaseInhibitorinhibitorinhibit

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