1. Apoptosis Autophagy
  2. Apoptosis Autophagy MDM-2/p53
  3. p53-MDM2-IN-5

p53-MDM2-IN-5 (compound 5a) is a potent p53-MDM2 inhibitor. p53-MDM2-IN-5 induces apoptosis, autophagy and DNA damage. p53-MDM2-IN-5 induces cell cycle arrest at S and G2/M phases. p53-MDM2-IN-5 shows anti-tumor activity.

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p53-MDM2-IN-5 Chemical Structure

p53-MDM2-IN-5 Chemical Structure

CAS No. : 2750075-06-8

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Description

p53-MDM2-IN-5 (compound 5a) is a potent p53-MDM2 inhibitor. p53-MDM2-IN-5 induces apoptosis, autophagy and DNA damage. p53-MDM2-IN-5 induces cell cycle arrest at S and G2/M phases. p53-MDM2-IN-5 shows anti-tumor activity[1].

In Vitro

p53-MDM2-IN-5 (compound 5a) (1-5 µM; 24 h) induces apoptosis and cell cycle arrest at S and G2/M phases in A549 cells[1].
p53-MDM2-IN-5 (1, 5 µM; 24 h) induces autophagy by decreases the expression of SQSTM1/p62[1].

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

Cell Viability Assay[1]

Cell Line: A549, A549/CDDP, Panc-1, CFPAC-1, SJSA-1, HepG2, HCT116, HLF-1 cells
Concentration: 0-100 µM
Incubation Time: 24 h
Result: Inhibited cell growth with IC50s of 0.85, 1.43, 2.22, 1.64, 0.14, 6.23, 2.57, 18.94 µM for A549, A549/CDDP, Panc-1, CFPAC-1, SJSA-1, HepG2, HCT116, HLF-1 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 1 µM
Incubation Time: 24 h
Result: Induced cell cycle arrest at S and G2/M phases.

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 0.1, 0.5, 1 µM
Incubation Time: 24 h
Result: Induced apoptosis with the percentages of apoptotic cells of 8.1%, 11.4%, and 15.1% at 0.1, 0.5, 1 µM, respectively.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 1, 5 µM
Incubation Time: 24 h
Result: Induced autophagy by promoted the conversion of LC3B-I to LC3B-II and decreased the expression of SQSTM1/p62.
In Vivo

p53-MDM2-IN-5 (6 μmol/kg; i.v.; every 3 days for 21 days) shows anti-tumor activity in A549 xenograft nude mouse model[1].

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

Animal Model: 6–8-week-old female nude mouse (A549 xenograft nude mouse model)[1]
Dosage: 6 μmol/kg
Administration: I.v.; every 3 days for 21 days
Result: Inhibited tumor growth with low toxicity.
Molecular Weight

974.57

Formula

C33H37Cl4F2N5O6Pt

CAS No.
SMILES

N#C[C@@]1(C2=C(C=C(C=C2)Cl)F)[C@@H](C3=C(C(Cl)=CC=C3)F)[C@@H](N[C@H]1CC(C)(C)C)C(NC4=C(C=C(C=C4)C([O-][Pt+4]([Cl-])([Cl-])([NH3])([NH3])[O-]C(C)=O)=O)OC)=O

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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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