1. Apoptosis
  2. MDM-2/p53

MDM-2/p53

Activation of the p53 protein protects the organism against the propagation of cells that carry damaged DNA with potentially oncogenic mutations. MDM2, a p53-specific E3 ubiquitin ligase, is the principal cellular antagonist of p53, acting to limit the p53 growth-suppressive function in unstressed cells. In unstressed cells, MDM2 constantly monoubiquitinates p53 and thus is the critical step in mediating its degradation by nuclear and cytoplasmic proteasomes. The interaction between p53 and MDM2 is conformation-based and is tightly regulated on multiple levels. Disruption of the p53-MDM2 complex by multiple routes is the pivotal event for p53 activation, leading to p53 induction and its biological response. Because the p53-MDM2 interaction is structurally and biologically well understood, the design of small lipophilic molecules that disrupt or prevent it has become an important target for cancer therapy.

MDM-2/p53 Related Products (41):

Cat. No. Product Name Effect Purity
  • HY-15676
    RG7388 Antagonist 99.97%
    RG7388 is a potent and selective p53-MDM2 antagonist with IC50 of 6 nM.
  • HY-15484
    Pifithrin-α hydrobromide Inhibitor 98.28%
    Pifithrin-α hydrobromide is an inhibitor of p53, also acts as an aryl hydrocarbon receptor (AhR) agonist.
  • HY-32735
    Triptolide Inhibitor 99.83%
    Triptolide is an inhibitor of heat shock factor (HSF1), inhibits HSP90-CDC37 binding and induces acetylation of HSP90, and also inhibits MDM2 expression in a dose-dependent manner with IC50 values range from 47 to 73 nM.
  • HY-10029
    Nutlin 3a Inhibitor 98.11%
    Nutlin (3a) is a murine double minute (MDM2) antagonist that inhibits MDM2-p53 interactions and stabilizes the p53 protein, thereby inducing cell cycle arrest and apoptosis.
  • HY-12296
    AMG 232 Inhibitor 99.73%
    AMG 232 is an extremely potent inhibitor of p53-MDM2 interaction (SPR Kd=0.045 nM, SJSA-1 EdU IC50=9.1 nM).
  • HY-18935A
    CBL0137 hydrochloride Activator 98.25%
    CBL0137 hydrochloride is an inhibitor of the histone chaperone, FACT. CBL0137 hydrochloride can also activate p53 and inhibits NF-κB with EC50s of 0.37 and 0.47 µM, respectively.
  • HY-19896
    COTI-2 Activator 99.40%
    COTI-2 is a small molecule candidate anti-cancer drug which can convert mutant p53 to wild-type conformation.
  • HY-103640
    WR-1065 dihydrochloride Activator
    WR-1065 dihydrochloride can protect normal tissues from the toxic effects of certain cancer drugs and activate p53 through a JNK-dependent signaling pathway.
  • HY-15695
    Puromycin aminonucleoside Activator 98.31%
    Puromycin aminonucleoside is the aminonucleoside portion of the antibiotic puromycin, and a puromycin analog which does not inhibit protein synthesis or induce apoptosis.
  • HY-10959
    RG7112 Inhibitor 99.94%
    RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2, with the Kd value of 11 nM.
  • HY-15954
    NVP-CGM097 Inhibitor 98.32%
    NVP-CGM097 is a potent and selective MDM2 inhibitor with IC50 of 1.7±0.1 nM for hMDM2.
  • HY-16702A
    Pifithrin-β hydrobromide Inhibitor 99.90%
    Pifithrin-β is a potent p53 inhibitor with an IC50 of 23 μM.
  • HY-50696
    Nutlin 3 Inhibitor 98.32%
    Nutlin 3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.
  • HY-16664
    SJ-172550 Inhibitor 99.44%
    SJ-172550 is a small molecule inhibitor of MDMX; competes for the wild type p53 peptide binding to MDMX with an EC50 of 5 μM.
  • HY-15510B
    Tenovin 6 Hydrochloride Activator >98.0%
    Tenovin-6 Hydrochloride is a water soluble inhibitor of SIRT1 and SIRT2, slightly inhibits HDAC8, and is also a potent activator of p53, with IC50s of 21 μM, 10 μM, 67 μM for SirT1, SirT2, and SirT3, respectively.
  • HY-18986
    SAR405838 Inhibitor 98.95%
    SAR405838 is a highly potent and selective MDM2 inhibitor, binds to MDM2 with Ki= 0.88 nM and has high specificity over other proteins.
  • HY-13424
    RITA Inhibitor
    RITA(NSC 652287) induced both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks.
  • HY-P0121
    ReACp53 Inhibitor 99.65%
    ReACp53 is cell-penetrating peptide, designed to inhibit p53 amyloid formation, rescues p53 function in cancer cell lines and in organoids derived from high-grade serous ovarian carcinomas (HGSOC).
  • HY-13423
    Tenovin-1 Activator 99.39%
    Tenovin-1 is an inhibitor of sirtuin 1 and sirtuin 2, an activator of p53 and may have potential in the management of cancer.
  • HY-17493
    MI-773 Inhibitor >98.0%
    MI-773 is a new small molecule inhibitor of the MDM2-p53 interaction, binds to MDM2 with high affinity (Ki=0.88 nM) and blocks the p53-MDM2 interaction.