MDM2/4-p53-IN-2

Cat. No.: HY-151170: FAQs
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MDM2/4-p53-IN-2 (2q) is a potent dual MDM2/ MDM4 inhibitor and p53 activator with the IC₅₀ values of 70.7 nM for MDM2- p53 and 81.4 nM for MDM4-p53 complexes. MDM2/4-p53-IN-2 regulates the cell cycle, induces cell apoptosis and has anticancer activity.

For research use only. We do not sell to patients.

MDM2/4-p53-IN-2 Chemical Structure

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Description

In Vitro

MDM2/4-p53-IN-2 (2q) (1-100 μM, 96 h) can inhibit the proliferation of cancer cells and induce cell apoptosis by targeting the G0/G1 cell cycle in a dose-dependent manner^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	Human cancer cell lines HCT116, SJSA-1, MCF-7, LNCaP, human embryonic kidney epithelial cell line HEK 293T
Concentration:	1-100 μM
Incubation Time:	48 hours
Result:	Showed anti-proliferative activity of HCT116 with an IC₅₀ value of 18.0 μM. Showed well inhibition of cell viability against SJSA-1, MCF-7, LNCaP cells, all below 40%. Reduced cell viability of HEK 293T cells by 24%.

Apoptosis Analysis^[1]

Cell Line:	SJSA-1 cell lines
Concentration:	15 and 22.5 μM
Incubation Time:	96 hours
Result:	Increased LDH release by 1.3-fold and 1.6-fold at concentrations of 15 μM and 22.5 μM, respectively. Caused a decrease in SJSA-1 cells, a significant decrease in cell growth and an increase in the number of early and late stage apoptotic cells at 22.5 μM. Induced a significant accumulation of G0/G1 phase cells with a percentage of 67.5% at 15 μM and 82.2% at 22.5 μM, while reducing the percentage of S and G2/M phase cells.

Molecular Weight

532.78

Formula

C₂₅H₁₇Cl₃FN₃O₃

SMILES

O=C(C([C@@H]1C2=CC=CC(Cl)=C2F)=NN(C3=CC=C(Cl)C=C3)[C@@]41C(NC5=C4C=CC(Cl)=C5)=O)OCC.[Relative stereochemistry]

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

Handling Instructions (2659 KB)

References

[1]. Margarida Espadinha, et al. Discovery of MDM2-p53 and MDM4-p53 protein-protein interactions small molecule dual inhibitors. Eur J Med Chem. 2022 Aug 5;241:114637. [Content Brief]

MDM2/4-p53-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:

MDM2/4-p53-IN-2MDM-2/p53ApoptosisMDM2MDM4p53anticancerapoptosiscell cycleInhibitorinhibitorinhibit

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