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Results for "

y220c

" in MedChemExpress (MCE) Product Catalog:

23

Inhibitors & Agonists

1

Isotope-Labeled Compounds

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-148416
    p53 Activator 7
    1 Publications Verification

    		 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-108637
    PhiKan 083
    1 Publications Verification

    		 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-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-169369
    TRAP-1

    XJZ-06-462

    		 MDM-2/p53 Apoptosis Cancer
    TRAP-1 (XJZ-06-462) is a non-covalent regulated induced proximity targeting chimera (RIPTAC) with JQ-1 carboxylic acid (HY-78695) as its target protein ligand. TRAP-1 forms a ternary complex with p53 Y220C and BRD4, potently activates p53 transcription, and inhibits the growth and proliferation of tumor cells. TRAP-1 upregulates p21 and other p53 target genes in pancreatic cell lines carrying p53 Y220C, and induces cellular senescence and apoptosis. TRAP-1 can be used in cancer research involving p53 Y220C-carrying tumors .
    TRAP-1
  • 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-180619
    p53 Y220C ligand-1

    		MDM-2/p53 Cancer
    p53 Y220C ligand-1(compound PK-A) is a target protein ligand of p53 DUBTAC modulator-1 (HY-180618). p53 Y220C ligand-1 exhibits potent activity in inhibiting cell proliferation in Huh7 cells .
    p53 Y220C ligand-1
  • 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-175318S
    p53 Activator 15

    		MDM-2/p53 Cancer
    p53 Activator 15 is an orally active p53 Y220C activator. p53 Activator 15 enhances the DNA binding of p53 Y220C (SC50 = 0.58 nM) and significantly inhibits NUGC-3 cell proliferation. p53 Activator 15 effectively inhibits tumor growth in NUGC-3 xenograft mouse and rat models. p53 Activator 15 can be used to study gastric cancer .
    p53 Activator 15
  • 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-108637A
    PhiKan 083 hydrochloride
    1 Publications Verification

    		 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-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-181616
    p53-Y220C/PLK1 modulator-1

    		MDM-2/p53 Polo-like Kinase (PLK) Cancer
    p53-Y220C/PLK1 modulator-1 (compound15) is a dual modulator targeting p53-Y220C and PLK1. p53-Y220C/PLK1 modulator-1 can be used in the cancer .
    p53-Y220C/PLK1 modulator-1
  • HY-W287494
    Antitumor agent-202

    		MDM-2/p53 Cancer
    Antitumor agent-202 is a stabilizer of the p53 Y220C mutant. It exhibits a selective inhibitory effect on the proliferation of tumor cells carrying the p53 Y220C mutation and can be applied to the research of cancers associated with the p53 Y220C mutation .
    Antitumor agent-202
  • HY-100601
    PK7242

    		MDM-2/p53
    PK7242 is an inducer of reactivation of mutant p53 in cancer cells. In cancer cells carrying the Y220C mutant, PK7242 binds to the p53-Y220C core domain and induces growth inhibition, cell-cycle arrest, and apoptosis.
    PK7242
  • HY-182744
    LLQ-45

    		MDM-2/p53 Cancer
    LLQ-45 is a covalent p53 Y220C mutant protein agonist with an EC50 of 24.97 μM. LLQ-45 activates the anti-tumor function of p53 Y220C through covalent modification, restores its DNA-binding ability and enhances its thermal stability. LLQ-45 selectively inhibits the proliferation of p53 Y220C mutant tumor cells, suppresses cell growth and upregulates the expression of CDKN1A. LLQ-45 can be used in studies related to p53 Y220C mutant cancers .
    LLQ-45
  • HY-179507
    p53 Activator 17

    		MDM-2/p53 Apoptosis Cancer
    p53 Activator 17 is a p53-Y220C activator. p53 Activator 17 exhibits selective cytotoxicity and pro-apoptotic activity in p53-Y220C mutant cancer cell lines, with minimal effects in wild-type or p53-null cells. p53 Activator 17 induces a mutant-to-wild-type conformational shift in cellular p53-Y220C, accompanied by transcriptional activation of canonical p53 target genes, including BBC3 (PUMA) and MDM2. p53 Activator 17 can be used for the study of hepatocellular carcinoma and breast cancer .
    p53 Activator 17
  • HY-180618
    p53 DUBTAC modulator-1

    		MDM-2/p53 Apoptosis Bcl-2 Family Wnt Cancer
    p53 DUBTAC modulator-1 (Compound A1) is a p53 Y220C DUBTAC modulator (Kd = 12.09 µM). p53 DUBTAC modulator-1 effectively reactivates and deubiquitinates mutant p53 Y220C. p53 DUBTAC modulator-1 upregulates p53 Y220C protein levels. p53 DUBTAC modulator-1 induces Apoptosis, reduces Bcl-2, inhibits Wnt signaling. p53 DUBTAC modulator-1 has anti-cancer activity against liver cancer .
    p53 DUBTAC modulator-1
  • HY-179506
    p53 Activator 16

    		MDM-2/p53 Apoptosis Cancer
    P53 Activator 16 (Compound JC16) is a p53 activator. P53 Activator 16 exhibits selective cytotoxicity and pro-apoptotic (apoptosis) activity towards p53-Y220C mutant cancer cells, while having little effect on wild-type or P53-deficient cells. P53 Activator 16 induces the conformational transition of cell p53-Y220C from the mutant form to the wild-type form, accompanied by the transcriptional activation of p53 target genes, without increasing the overall level of p53 protein. P53 Activator 16 can be used for the study of p53 mutant cancers .
    p53 Activator 16
  • HY-119408
    MB725

    		MDM-2/p53 Bcl-2 Family Cancer
    MB725 is an ethylamide analogue of MB710 (HY-120373). MB725 increases mRNA levels of a range of p53 target genes, notably PUMA, p21, MDM2, NOXA and BAX. MB725 shows selective anticancer activity against p53-Y220C cancer .
    MB725
  • 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
  • HY-108637R
    PhiKan 083 (Standard)

    		Reference Standards MDM-2/p53 Cancer
    PhiKan 083 (Standard) is the analytical standard of PhiKan 083 (HY-108637). This product is intended for research and analytical applications. 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 (Standard)
  • HY-186101
    P53 mutant stabilizer-1

    		MDM-2/p53 Cancer
    P53 mutant stabilizer-1 (compound 274) is a covalent mutant p53 stabilizer. P53 mutant stabilizer-1 can be used for the study of wild-type function of p53 mutants, such as cancers associated with p53 mutation .
    P53 mutant stabilizer-1

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