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p53 mutant

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-145759
    Mutant p53 modulator-1

    		MDM-2/p53 Cancer
    Mutant p53 modulator-1 is a mutant p53 modulator. Mutant p53 modulator-1 reduces the progression of cancers that contain a p53 mutation (extracted from patent WO2021231474A1, compound 231B) .
    Mutant p53 modulator-1
  • HY-153767
    PK095

    		MDM-2/p53 Cancer
    PK095 is a p53 mutant stabilizer. PK095 can be used for research of cancer .
    PK095
  • HY-19634
    YK-3-237

    		Sirtuin Cancer
    YK-3-237, a SIRT1 activator, targets mutant p53. YK-3-237 inhibits the proliferation of triple-negative breast cancer cells .
    YK-3-237
  • HY-156967
    BAY 1892005

    		MDM-2/p53 Cancer
    BAY 1892005 is a regulator of p53 protein and acts on p53 condensates without causing mutant p53 reactivation .
    BAY 1892005
  • HY-108636
    RETRA

    		MDM-2/p53 Cancer
    RETRA is a mutant p53-dependent activator of p73 that suppresses mutant p53-bearing cancer cells. RETRA increases the expression level of p73, and a release of p73 from the blocking complex with mutant p53, which produces tumor-suppressor effects .
    RETRA
  • HY-148404
    p53 Activator 5

    		MDM-2/p53 Cancer
    p53 Activator 5 (compound 134A) is a potent p53 activator with a SC150 value of <0.05 mM. p53 Activator 5 can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA. p53 Activator 5 shows anti-tumor activity . p53 Activator 5 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 5
  • HY-148402
    p53 Activator 3

    		MDM-2/p53 Cancer
    p53 Activator 3 (compound 87A) is a potent p53 activator with a SC150 value of <0.05 mM. p53 Activator 3 can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA. p53 Activator 3 shows anti-tumor activity . p53 Activator 3 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 3
  • 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-N10502
    Colletofragarone A2

    		MDM-2/p53 HSP Cancer
    Colletofragarone A2 can be be isolated from the fungus Colletotrichum sp. (13S020). Colletofragarone A2 inhibits mutant p53 and HSP90 with anti-cancer activity. Colletofragarone A2 promotes degradation and aggregation of mutant p53 and suppressing tumor growth in vivo .
    Colletofragarone A2
  • HY-158151
    p53 Activator 12

    		MDM-2/p53 Cancer
    p53 Activator 12 (compound 510B) is a potent p53 activator. p53 Activator 12 binds to mutant p53 and restores the ability of the p53 mutant to bind DNA .
    p53 Activator 12
  • HY-19726
    NSC59984
    1 Publications Verification

    		 MDM-2/p53 Cancer
    NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway . NSC59984 acts by targeting GOF-mutant p53 and stimulates p73 to restore the p53 pathway signaling .
    NSC59984
  • HY-18343A
    CP-31398 dihydrochloride

    		MDM-2/p53 Cancer
    CP-31398 dihydrochloride stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53 .
    CP-31398 dihydrochloride
  • HY-113843
    RETRA hydrobromide

    		Others Cancer
    RETRA (hydrobromide) is a mutant p53-dependent activator of p73 that can inhibit cancer cells carrying mutant p53. RETRA (hydrobromide) increases the expression level of p73, induces transcriptional activation of several common to transcriptional targets p53 and p73, which leads to mutant p53- and p73-dependent inhibition of tumor growth, reduction of colony formation and induction of effector caspases .
    RETRA hydrobromide
  • 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-144104
    NSC90616

    		MDM-2/p53 Cancer
    NSC90616 is a mutant p53 rescue compound .
    NSC90616
  • HY-19896
    COTI-2
    2 Publications Verification

    		 MDM-2/p53 Apoptosis Cancer
    COTI-2, an anti-cancer agent with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation .
    COTI-2
  • HY-159493
    BI2536-PEG2-Halo

    		Polo-like Kinase (PLK) Cancer
    BI2536-PEG2-Halo is a bifunctional molecule containing a ligand for Halo tag and a Polo-like kinase 1 (PLK1) inhibitor BI-2536 (HY-50698). BI2536-PEG2-Halo inhibits the proliferation of 293T cells with Halo-p53R273H(FL)-mCherry tag (IC50=23 nM), exhibits selective toxicity against p53 mutant cancer cells .
    BI2536-PEG2-Halo
  • HY-122578
    P53R3

    		MDM-2/p53 Cancer
    P53R3 is a potent p53 reactivator and restores sequence-specific DNA binding of p53 hot spot mutants, including p53 R175H, p53 R248W and p53 R273H. P53R3 induces p53-dependent antiproliferative effects with much higher specificity than PRIMA-1. P53R3 enhances the recruitment of wild-type p53 and p53 M237I to several target gene promoters. P53R3 strongly enhances the mRNA, total protein and cell surface expression of the death receptor death receptor 5 (DR5). P53R3 is used for cancer research .
    P53R3
  • HY-145785
    ADH-6

    		MDM-2/p53 Apoptosis Cancer
    ADH-6 is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 has the potential for the research of cancer diseases[1].
    ADH-6
  • HY-145785A
    ADH-6 TFA

    		MDM-2/p53 Apoptosis Cancer
    ADH-6 TFA is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 TFA targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 TFA has the potential for the research of cancer diseases .
    ADH-6 TFA
  • HY-108639
    MIRA-1

    NSC 19630

    		 MDM-2/p53 Apoptosis Cancer
    MIRA-1 is a maleimide analogue. MIRA-1 can induce apoptosis in mutant p53 cells via restoration of p53-dependent transcriptional transactivation. MIRA-1 has anticancer activity .
    MIRA-1
  • HY-110088
    SCH529074
    1 Publications Verification

    		 MDM-2/p53 Cancer
    SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC) .
    SCH529074
  • HY-P10610
    Peptide 234CM

    		MDM-2/p53 Cancer
    Peptide 234CM is a peptide containing isoleucine at position 3, corresponding to the sequence of a point mutation in p53 codon 234. Peptide 234CM induces potent cytotoxic T cell (CTL) and antitumor immune responses against mutant p53 .
    Peptide 234CM
  • HY-120667
    DS-5272

    		MDM-2/p53 Apoptosis Cancer
    DS-5272 is an orally acitve inhibitor for p53-MDM2 with an IC50 of 20 nM. DS-5272 inhibits the proliferation of SJSA-1 (wildtype p53, IC50=0.17 μM) and DLD-1 (mutant p53). DS-5272 arrest the cell cycle, and induces apoptosis in SJSA-1. DS-5272 exhibits antitumor efficacy in mice .
    DS-5272
  • HY-U00447
    PK11000

    		MDM-2/p53 DNA Alkylator/Crosslinker Cancer
    PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding. PK11000 has anti-tumor activities .
    PK11000
  • HY-18634
    NSC319726
    1 Publications Verification

    ZMC1

    		 MDM-2/p53 Cancer
    NSC319726 (ZMC1) is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.
    NSC319726
  • HY-13811
    NSC697923
    1 Publications Verification

    		 E1/E2/E3 Enzyme Apoptosis Cancer
    NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity .
    NSC697923
  • HY-19980A
    PRIMA-1
    2 Publications Verification

    NSC-281668

    		 Autophagy MDM-2/p53 Ferroptosis Apoptosis Cancer
    PRIMA-1 (NSC-281668) is a mutant p53 reactivator, restores the sensitivity of TP53 mutant-type thyroid cancer cells to the histone methylation inhibitor 3-Deazaneplanocin A.
    PRIMA-1
  • HY-128784
    PK11007

    		MDM-2/p53 Reactive Oxygen Species Cancer
    PK11007 is a mild thiol alkylator with anticancer activity. PK11007 stabilizes p53 via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity. PK11007 induces mutant p53 cancer cell death by increasing reactive oxygen species (ROS) levels .
    PK11007
  • HY-148409
    MMRi62

    		Ferroptosis Apoptosis Autophagy MDM-2/p53 Cancer
    MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .
    MMRi62
  • HY-136910
    USP7-797

    USP7-IN-7

    		 Deubiquitinase MDM-2/p53 Cancer
    USP7-797 (USP7-IN-7) is an orally available, selective USP7 inhibitor (IC50=0.5 nmol/L) with antitumor activity. USP7-797 reduces the level of MDM2, thereby increasing the stability and activity of p53, leading to cell cycle arrest and apoptosis. USP7-797 has low nanomolar cytotoxicity against p53 mutant cancer cell lines, p53 wild-type hematological tumors, and neuroblastoma cell lines .
    USP7-797
  • 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-16271
    Kevetrin hydrochloride
    1 Publications Verification

    4-Isothioureidobutyronitrile hydrochloride; thioureidobutyronitrile hydrochloride; thioureido butyronitrile hydrochloride

    		 MDM-2/p53 Apoptosis Cancer
    Kevetrin hydrochloride is a potent activator of p53, induces apoptosis in TP53 wild-type and mutant acute myeloid leukemia cells. Kevetrin a preferential cytotoxic activity against blast cells .
    Kevetrin hydrochloride
  • HY-120122
    PK7088

    		Others Cancer
    PK7088 is a pyrazole and a specific peptide. PK7088 supports the reactivation of mutant p53 by converting it to a form exhibiting wild-type properties. PK7088 exhibit anticancer activity in cancer research .
    PK7088
  • HY-130122
    MG-277

    		Molecular Glues PROTACs Apoptosis Cancer
    MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon E3 ligand, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity .
    MG-277
  • 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-B0282
    Acetylcholine chloride
    Maximum Cited Publications
    11 Publications Verification

    ACh chloride

    		 nAChR Calcium Channel Endogenous Metabolite Neurological Disease Cancer
    Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
    Acetylcholine chloride
  • 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-19980
    Eprenetapopt
    5+ Cited Publications

    APR-246; PRIMA-1Met

    		 MDM-2/p53 Autophagy Apoptosis Ferroptosis Cancer
    Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance .
    Eprenetapopt
  • HY-158684
    YX-02-030

    		PROTACs MDM-2/p53 Cancer
    YX-02-030M is a PROTAC MDM2 degrader. YX-02-030M inhibits MDM2-p53 binding and VHL-HIF1α binding with IC50s of 63 nM and 1.35 μM respectively. YX-02-030M binds MDM2 and recruits the VHL E3 ubiquitin ligase to initiate MDM2 degradation, and effectively kills p53 mutant or deleted Triple-negative breast cancers (TNBC) cells. (Blue: VHL ligand; Black: linker; Pink: MDM2 inhibitor) .
    YX-02-030
  • 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-B0282S
    Acetylcholine-d4 chloride

    ACh-d4 (chloride)

    		 nAChR Calcium Channel Endogenous Metabolite Neurological Disease Cancer
    Acetylcholine-d4 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs)[1][2]. Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro[5].
    Acetylcholine-d4 chloride
  • HY-B0282S1
    Acetylcholine-d9 chloride

    ACh-d9(chloride)

    		 nAChR Calcium Channel Endogenous Metabolite Neurological Disease Cancer
    Acetylcholine-d9 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs)[1][2]. Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro[5].
    Acetylcholine-d9 chloride
  • HY-B0282R
    Acetylcholine chloride (Standard)

    		nAChR Calcium Channel Endogenous Metabolite Neurological Disease Cancer
    Acetylcholine (chloride) (Standard) is the analytical standard of Acetylcholine (chloride). This product is intended for research and analytical applications. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
    Acetylcholine chloride (Standard)
  • HY-122753
    SLMP53-1

    		MDM-2/p53 Cancer
    SLMP53-1 is a wild-type and mutant p53 reactivator with promising antitumor activity. SLMP53-1 mediates the reprograming of glucose metabolism in cancer cells. SLMP53-1 depletes angiogenesis, decreasing endothelial cell tube formation and vascular endothelial growth factor (VEGF) expression levels .
    SLMP53-1
  • HY-148369
    U7D-1

    		PROTACs Deubiquitinase Apoptosis MDM-2/p53 Cancer
    U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells. U7D-1 shows anticancer activity. U7D-1 induces apoptosis in Jeko-1 cells .
    U7D-1

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