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MDM2-p53-IN-16 is a MDM2-p53 complex inhibitor with an IC 50 value of 4.3 nM to dissociate human p53/MDM2 complex. MDM2-p53-IN-16 reactivates p53, and induces Glioblastoma Multiforme (GBM) cell apoptosis and cell-cycle arrest. MDM2-p53-IN-16 can be used for the cancer research.
In Vitro
MDM2-p53-IN-16 (0.01 nM-100 μM; 1 hour) dissociates MDM2-p53 interaction with an IC 50 value of 4.3 nM. MDM2-p53-IN-16 (1 µM; 8 hours) significantly increases the levels of p53 in GBM cells. MDM2-p53-IN-16 (1 µM; 6 hours) increases the mRNA levels of p53 target genes: MDM2, PUMA and p21 in U87MG cells. MDM2-p53-IN-16 binds with translocator protein (TSPO) with a K i value of 87.2 nM. MDM2-p53-IN-16 (1 µM; 24 hours) induces early and late apoptosis and cell cycle arrest of U87MG cells. MDM2-p53-IN-16 (1-10000 nM; 48 h) shows antiproliferative activities to U87MG and wild-type p53 U343MG cells with IC 50 values of 1.2 and 1.6 μM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: U87MG, U343MG and T98G cell lines Concentration: 1-10000 nM Incubation Time: 48 hours Result: Inhibited cell proliferation of U87MG, U343MG and T98G cells. Apoptosis AnalysisCell Line: U87MG cell line Concentration: 1 µM Incubation Time: 24 hours Result: Induced cell apoptosis of U87MG cells. Cell Cycle AnalysisCell Line: U87MG, U343MG and T98G cell lines Concentration: 1-10000 nM Incubation Time: 48 hours Result: Induced cell cycle arrest progression in the G2/M-phase of U87MG cells.
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