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TP53Y220C

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-156633
    Rezatapopt
    3 Publications Verification

    PC14586

    		 MDM-2/p53 Cancer
    Rezatapopt (PC14586) is an orally active antineoplastic agent. Rezatapopt binds to a pocket created by the TP53 Y220C mutation. Rezatapopt restores p53 tumor suppressor functions by stabilization of the p53 protein structure. Rezatapopt demonstrates tumor inhibition and regression in mouse models with established human tumor xenografts harboring the TP53 Y220C mutation .
    Rezatapopt
  • HY-179560
    PMV6-PEG4-BI2536

    		Polo-like Kinase (PLK) MDM-2/p53 Cancer
    PMV6-PEG4-BI2536 is a p53-Y220C-PLK1 dual-functional compound, composed of a high-affinity p53-Y220C mutant binder (Kd ≈ 2.5 nM) and a potent PLK1 kinase inhibitor (IC50 = 0.83 nM). PMV6-PEG4-BI2536 triggers TP53 Y220C cell G2/M arrest and apoptosis through PLK1 mislocalization and kinase inhibition, independent of p53 transcriptional reactivation. PMV6-PEG4-BI2536 can be used for the study of TP53 mutant cancers .
    PMV6-PEG4-BI2536
  • HY-164828
    Rezatapopt analog-1

    PC14586 analog-1

    		 MDM-2/p53 Cancer
    Rezatapopt analog-1 (PC14586 analog-1) (1919) is a Rezatapopt (HY-156633) analog. Rezatapopt binds to a pocket created by the TP53 Y220C mutation. Rezatapopt restores p53 tumor suppressor functions by stabilization of the p53 protein structure .
    Rezatapopt analog-1

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