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p53 Y220C

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-120373
    MB710
    1 Publications Verification

    		 MDM-2/p53 Cancer
    MB710, an aminobenzothiazole derivative, is a stabilizer of oncogenic p53 mutation Y220C. MB710 binds tightly to the Y220C pocket and stabilizes p53-Y220C, with a Kd of 4.1 μM. MB710 shows anticancer activity in p53-Y220C cell lines .
    MB710
  • HY-148416
    p53 Activator 7

    		MDM-2/p53 Cancer
    p53 Activator 7 is a p53 mutation Y220C (MDM-2/p53) activator with an EC50 of 104 nM. p53 Activator 7 can bind to p53 mutant and restore its ability to bind DNA (WO2022213975A1; Example B-1) . p53 Activator 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    p53 Activator 7
  • HY-156633
    Rezatapopt

    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-108637
    PhiKan 083

    		MDM-2/p53 Cancer
    PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM. PhiKan 083 can be used for cancer research .
    PhiKan 083
  • HY-108637A
    PhiKan 083 hydrochloride

    		MDM-2/p53 Cancer
    PhiKan 083 hydrochloride is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM , and a relative binding affinity (Kd) of 150 μM in Ln229 cells .
    PhiKan 083 hydrochloride
  • HY-153202
    SLMP53-2

    		MDM-2/p53 Apoptosis Cancer
    SLMP53-2 is a mutant p53 reactivator. SLMP53-2 restores wild-type-like conformation and DNA-binding ability of mutp53-Y220C by enhancing its interaction with the Hsp70, leading to the reestablishment of p53 transcriptional activity. SLMP53-2 can induce cell cycle arrest, apoptosis and endoplasmic reticulum (ER) stress. SLMP53-2 exhibits antitumor activity .
    SLMP53-2
  • HY-149306
    MS78

    		Histone Acetyltransferase MDM-2/p53 Cancer
    MS78 is an acetylation targeting chimera (AceTAC) that acetylates the p53 tumor suppressor protein. MS78 recruits histone acetyltransferase p300/CBP to acetylate the p53Y220C mutant. MS78 upregulates TRAIL apoptotic genes and downregulates DNA damage response pathways. MS78 contains a CBP/p300 binder, a p53Y220C binder and a linker .
    MS78
  • HY-160449
    p53 Activator 10

    		MDM-2/p53 Cancer
    p53 Activator 10 (Example C-2) is a compound that targets the y220c mutant of p53. p53 Activator 10 activation is involved in the downstream effects of tumor suppression .
    p53 Activator 10
  • HY-159606
    MS182

    		MDM-2/p53 Cancer
    MS182 (compound 11) is an acetylation targeting chimera (AceTAC) designed based on p53 Y220C stabilizer and targeting p53 Y220C. MS182 is composed of p53 Y220C and p300/CBP binders, respectively, coupled by a linker. MS182 forms a ternary complex with p300/CBP acetyltransferase and p53 Y220C in a time- and concentration-dependent manner, effectively acetylating lysine at position 382 of p53 Y220C (ACE50: 1.52 μM). MS182 also exhibited considerable bioavailability in mice, with GI50 values of 2.16 μM and 1.83 μM for BxPC3 (p53 Y220C/-) and NUGC (p53 Y220C/+), respectively .
    MS182
  • HY-160450
    p53 Activator 11

    		MDM-2/p53 Cancer
    p53 Activator 11 (compound A-1) is a potent p53 activator with an EC50 value of 0.478 µM for p53 (Y220C). p53 Activator 11 has the potential for the research of cancer .
    p53 Activator 11
  • HY-169369
    TRAP-1

    XJZ-06-462

    		 MDM-2/p53 Autophagy Apoptosis Cancer
    TRAP-1 (XJZ-06-462) is ap53 transcriptional activator that effectively activates mutant p53 and triggers the transcription of p53 target genes. TRAP-1 rapidly upregulates p21 and other p53 target genes in pancreatic cell lines with p53Y220C. TRAP-1 inhibits cell proliferation, with IC50 values of 3.94 and 0.531 μM in BxPC-3 and A549 cells, respectively. TRAP-1 regulates autophagy in lung cancer cells and offers protective effects against oxidative stress and cell apoptosis .
    TRAP-1

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