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mutant p53

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0282
    Acetylcholine chloride
    20+ Cited Publications

    ACh chloride

    		 nAChR Calcium Channel Endogenous Metabolite Infection Neurological Disease Cancer
    Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable 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-19980
    Eprenetapopt
    10+ 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-19896
    COTI-2
    4 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-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 and BBB-permeable 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-d4 chloride
  • 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-13811
    NSC697923
    5+ Cited Publications

    		 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-19726
    NSC59984
    2 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-145759
    Mutant p53 modulator-1
    1 Publications Verification

    		 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-110088
    SCH529074
    3 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-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-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-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-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-128784
    PK11007

    		MDM-2/p53 Reactive Oxygen Species (ROS) 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-16271
    Kevetrin hydrochloride
    4 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-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
    2 Publications Verification

    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-18634
    NSC319726
    3 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-N2445
    Flavokawain C
    4 Publications Verification

    		 Apoptosis Akt JNK PERK Caspase PARP MDM-2/p53 IAP Reactive Oxygen Species (ROS) SOD FABP Autophagy AMPK mTOR GLUT EGFR PI3K HSP VEGFR FAK Cancer
    Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer .
    Flavokawain C
  • 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-130122
    MG-277
    1 Publications Verification

    		 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-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 and BBB-permeable 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-d9 chloride
  • 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-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-120122
    PK7088

    		MDM-2/p53 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-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-B0282R
    Acetylcholine chloride (Standard)

    ACh chloride (Standard)

    		 Reference Standards 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 and BBB-permeable 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
  • 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
    1 Publications Verification

    		 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-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-126905
    ZMC3

    NSC328784

    		 Reactive Oxygen Species (ROS) Cancer
    ZMC3 (NSC328784) is a zinc chelator. ZMC3 shows Zinc metallochaperone properties. ZMC3 shows enhanced sensitivity in p53-R175H mutant cells. ZMC3 increases the cell ROS level .
    ZMC3
  • HY-174458
    MD-4251

    		PROTACs MDM-2/p53 IKZF Family Casein Kinase Cancer
    MD-4251 is an orally active MDM2 PROTAC degrader. MD-4251 potently degrades MDM2 in RS4;11 cells (DC50: 0.2 nM) and actives p53. MD-4251 shows strong antiproliferative activity against acute leukemia cells (wild-type p53) with minimal efficacy in mutant type. MD-4251 induces complete tumor regression in RS4;11 xenograft mice model . Pink: MDM2 ligand (HY-130684); Blue: CRBN ligase ligand (HY-W883326); Black: linker
    MD-4251
  • 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-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
  • 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-P10610A
    Peptide 234CM TFA

    		MDM-2/p53 Cancer
    Peptide 234CM TFA is a peptide containing isoleucine at position 3, corresponding to the sequence of a point mutation in p53 codon 234. Peptide 234CM TFA induces potent cytotoxic T cell (CTL) and antitumor immune responses against mutant p53 .
    Peptide 234CM TFA
  • 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-176916
    Mutant p53 modulator-2

    		MDM-2/p53 Cancer
    Mutant p53 modulator-2 (Compound 1988) is a mutant p53 modulator. Mutant p53 modulator-2 can be used in the research of cancer .
    Mutant p53 modulator-2
  • HY-W034419
    STIMA-1

    		MDM-2/p53 Apoptosis Cancer
    STIMA-1 can stimulate mutant p53 DNA binding in vitro and induce expression of p53 target proteins and trigger apoptosis in mutant p53-expressing human tumor cells .
    STIMA-1
  • HY-113843
    RETRA hydrobromide

    		MDM-2/p53 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-124070
    ISA 27

    		MDM-2/p53 Cancer
    ISA 27 is a small-molecule MDM2-p53 protein-protein interaction inhibitor. ISA 27 inhibits MDM2-mediated p53 ubiquitination and degradation. ISA 27 is promising for research of p53-mutant solid tumors (e.g., thyroid, breast cancer) .
    ISA 27
  • HY-18343
    CP-31398

    		MDM-2/p53 Apoptosis Cancer
    CP-31398 can stabilize the active conformation of p53 and promote p53 activity in cancer cells with either mutant or wild-type p53. In addition, CP-31398 can upregulate p53 target genes, such as p21WAF1/Cip1 and KILLER/DR5. CP-31398 exerts an inhibitory effect on tumor growth .
    CP-31398
  • 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-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-112347
    Isogranulatimide

    		Checkpoint Kinase (Chk) Cancer
    Isogranulatimide is a selective checkpoint kinase 1 (Chk1) inhibitor with an IC50 value of 0.1 μM. Isogranulatimide inhibits the G2/M checkpoint and inhibits the growth of p53-mutant tumor cells. Isogranulatimide is promising for research of tumors associated with DNA damage response .
    Isogranulatimide

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