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p53

p53 activators and inhibitors act on the tumor suppressor p53, a transcription factor activated by cellular stress. In unstressed cells the ubiquitin ligase mouse double minute 2 (MDM2) keeps p53 levels low by promoting its degradation. RG7112 blocks the p53-MDM2 interaction, and SJ 172550 targets the related protein mouse double minute 4 (MDM4, also called MDMX). RITA binds p53 itself, while tenovin-1 and tenovin-6 raise cellular p53 levels. Tenovin-6 also inhibits the deacetylases sirtuin 1 and sirtuin 2 (SIRT1, SIRT2). Pifithrin-α hydrobromide works the other way, inhibiting p53-dependent transcription in cells exposed to genotoxic stress. Further compounds directed at MDM2 are listed in the neighboring MDM2 category.

1 Item

  • Rezatapopt
    Cat. No.
    A53794
    CAS No.
    2636846-41-6

    Rezatapopt

    Synonyms: PC14586

    Rezatapopt (PC14586) is a small-molecule ligand that specifically targets the mutated TP53 protein, particularly the Y220C variant. By binding to a unique pocket formed by this mutation, Rezatapopt restores the structural integrity and tumor suppressor functions of p53. This compound has shown promising antitumor activity, leading to tumor inhibition and regression in mouse models with established human tumor xenografts featuring the TP53 Y220C mutation, making it a valuable tool for cancer research targeting p53 dysfunction.

    In stock View Details
    1 mg
    $65.00
    5 mg
    $135.00
    All 6 sizes

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