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p53

Tumor protein p53, also known as p53, cellular tumor antigen p53 (UniProt name), the Guardian of the Genome, phosphoprotein p53, tumor suppressor p53, antigen NY-CO-13, or transformation-related protein 53 (TRP53), is any isoform of a protein encoded by homologous genes in various organisms, such as TP53 (humans) and Trp53 (mice). This homolog (originally thought to be, and often spoken of as, a single protein) is crucial in multicellular organisms, where it prevents cancer formation, and thus functions as a tumor suppressor. As such, p53 has been described as "the guardian of the genome" because of its role in conserving stability by preventing genome mutation.

  • Brigimadlin
    T699232095116-40-6
    Brigimadlin (BI 907828) is an orally active and highly potent E3 ubiquitin-protein ligase MDM2-p53 antagonist with antitumor activity.Brigimadlin can be used to study metastatic BTC, PDAC, lung adenocarcinoma, or bladder cancer.
    • $270
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  • C16 Ceramide
    T3756224696-26-2
    C16 Ceramide (Palmitoyl Ceramide) is a naturally occurring small molecule that activates p53 by directly and selectively binding to it.
    • $39
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  • Rotenone
    T297083-79-4
    Rotenone (Rotocide) is a natural product and a botanical insecticide. Rotenone is a mitochondrial electron transport complex I inhibitor that promotes the production of reactive oxygen species in mitochondria and induces apoptosis.
    • $42
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  • Isoliquiritin
    T5S03315041-81-6
    1. Isoliquiritin (Neoisoliquritin) has antitussive effects. 2. Isoliquiritin has antidepressant-like effects. 3. Isoliquiritin, liquiritin and isoliquirigenin inhibits the p53-dependent pathway and shows crosstalk between Akt activities.
    • $39
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  • Pifithrin-α hydrobromide
    T270763208-82-2
    Pifithrin-α hydrobromide (Pifithrin-α hydrobromide) is a p53 inhibitor, inhibiting p53-dependent transactivation of p53-responsive genes.
    • $33
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  • Eprenetapopt
    T44145291-32-7
    Eprenetapopt (PRIMA-1Met) restores wild-type conformation and function to mutant p53, and triggers apoptosis in tumor cells. PRIMA-1MET also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance.
    • $67
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  • Pinoresinol
    TN2080487-36-5
    Pinoresinol ((+)-Pinoresinol) has antiinflammatory, hepatoprotective, and fungicidal activities, it can protect pial microcirculation from I-reperfusion injury, to increase nitric oxide release and to reduce oxidative stress preserving pial blood flow distribution; it may exert pharmacologically interesting effects via modulation of the insulin-like signalling pathway in C.elegans. Pinoresinol causes an upregulation of the CDK inhibitor p21(WAF1 Cip1) both at mRNA and protein levels, inhibits NF-kappaB and activating protein 1 (AP-1).
    • $52
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  • Verbascoside
    T337561276-17-3
    Verbascoside (Kusaginin) is a protein kinase C inhibitor with antimicrobial, anti-inflammatory activities.
    • $58
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  • Rezatapopt
    T812892636846-41-6
    Rezatapopt (PC14586) is a small molecule p53 reactivator with anti-tumor activity that selectively binds to the cleft present in the TP53 Y220C mutant protein and restores the p53 wild-type (normal) conformation and transcriptional activity, and can be used to study locally advanced or metastatic solid tumors.
    • $970
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  • CBL0137 hydrochloride
    T43611197397-89-9
    CBL0137 hydrochloride (Curaxin-137 hydrochloride) activates p53 and inhibits NF-kB (EC50: 0.37 0.47 μM) in the cell-based p53 and NF-kB reporter assays, respectively. It also suppresses histone chaperone FACT.
    • $43
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  • Pifithrin-β hydrobromide
    T3637511296-88-1
    Pifithrin-β hydrobromide (Cyclic PFT-α) is an inhibitor of p53; reversibly blocks p53-dependent transcriptional activation and apoptosis. Protects against neuronal death in models of stroke and neurodegenerative disorders. Active in vivo; protects mice from the side-effects of Y therapy associated with p53 induction. Supresses self-renewal of embryonic stem cells. Also aryl hydrocarbon receptor (AHR) agonist, causes upregulation of AHR target gene CYP1A1 (EC50 = 1.1 μM).
    • $34
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  • HBX 41108
    T21527924296-39-9
    HBX 41108 (HBX-41108) is a non-competitive, reversible inhibitor of USP7 with an IC50 of 424nM. HBX 41108 inhibited deubiquitination of p53 mediated by USP7 in a dose-dependent manner with an IC50 of 0.8μM.
    • $47
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  • Pifithrin-μ
    T621064984-31-2
    Pifithrin-μ (NSC-303580) is an inhibitor of p53 and HSP70, with neuroprotective and antitumor activity.
    • $39
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  • Phenoxodiol
    T1652281267-65-4
    Phenoxodiol (Idronoxil) activates the mitochondrial caspase system, inhibits X-linked inhibitor of apoptosis(XIAP), disrupts FLICE inhibitory protein(FLIP) expression, and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol induces cell cycle arrest in the G1 S phase of the cell cycle and upregulates p21WAF1 via a p53 independent manner. Phenoxodiol also inhibits DNA topoisomerase II.
    • $60
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  • UC2288
    T96981394011-91-6
    UC2288 is a relatively selective p21 attenuator which is synthesized based Sorafenib. UC2288 attenuates p21 protein levels with minimal effect on p21 protein stability.
    • $41
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  • CBL0137
    T41261197996-80-7
    CBL0137 (Curaxin 137), a metabolically stable curaxin, activates p53 (EC50: 0.37 μM) and inhibits NF-κB (EC50: 0.47 μM). It functionally inactivates the facilitates chromatin transcription complex (FACT), driving the effects on p53 and NF-κB and promoting cancer cell death. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates the efficacy of gemcitabine in preClinicalal models of pancreatic cancer.
    • $44
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  • Moringin
    TN458373255-40-0
    Moringin is an isothiocyanate obtained from myrosinase-mediated hydrolysis of the glucosinolate precursor glucoMoringin present in Moringa oleifera seeds. Moringin has anti-inflammatory and antioxidative properties.
    • $138
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  • δ-Tocotrienol
    TMA247425612-59-3
    δ-Tocotrienol (Delta-Tocotrienol) is a potential angiogenic inhibitor. δ-Tocotrienol is also a nontoxic activator of mir-34a which can inhibit nonsmall cell lung cancer cells (NSC-LC) cell proliferation, induce apoptosis and inhibit invasion, and thus offering a potential starting point for the design of novel anticancer agents.
    • $40
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  • ZMC1
    T246471555-25-4
    NSC-319726 (ZMC1), a mutant p53R175 reactivator, suppresses growth of fibroblasts that expresses the p53R175 mutation (IC50 = 8 nM).
    • $32
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  • RO-5963
    T167711416663-77-8In house
    RO-5963 is a dual inhibitor of p53-MDM2 and p53-MDMX (IC50s: ~17 nM and ~24 nM, respectively).
    • $106
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  • Magnolol
    T3000528-43-8
    Magnolol (5,5'-Diallyl-2,2'-biphenyldiol) is a dual agonist of RXRα( EC50=10.4 μM) and PPARγ(EC50=17.7 μM). It blocks TNF-α-induced NF-KB activation.
    • $39
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  • Pifithrin-α, p-Nitro, Cyclic
    T1247260477-38-5
    Pifithrin-α, p-Nitro, Cyclic (PFN-α) is a cell-permeable, active-form inhibitor of p53.
    • $34
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  • Benzonitrile, 3,3'-[(2-oxo-1,3-cyclohexanediylidene)dimethylidyne]bis-
    T912963476-70-0
    Benzonitrile, 3,3'-[(2-oxo-1,3-cyclohexanediylidene)dimethylidyne]bis- is an inhibitor of p53 with an IC50 value of 0.35 μM
    • $44
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  • RITA
    T1798213261-59-7
    RITA (NSC-652287)(NSC-652287) induced cross-links of both DNA-DNA and DNA-protein with no detectable DNA single-strand breaks. RITA, like nutlin-3, can disrupt the p53/Mdm2 interaction.
    • $30
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  • Amifostine thiol dihydrochloride
    TQ013314653-77-1
    Amifostine thiol dihydrochloride (WR 1065) can activate p53 through a JNK-dependent signaling pathway. It also protects normal tissues from the toxic effects of certain cancer drugs.
    • $47
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  • p53-MDM2-IN-1
    T72026381717-91-5
    p53-MDM2-IN-1 (Example 30), an inhibitor of the p53-MDM2 X protein interaction, exhibits a K i value of 23.35 µM and holds potential for applications in anti-tumor research.
    • $195
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  • XI-006
    T661058131-57-0
    XI-006 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization activation and DNA damage, and also regulates MDM2, an E3 ligase.
    • $51
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  • Tenovin-6 Hydrochloride
    T84801011301-29-3
    Tenovin-6 Hydrochloride is an SIRT1, SIRT2 and HDAC8 inhibitor(IC50s of 21 μM, 10 μM, and 67 μM for SirT1, SirT2, and SirT3, respectively), and is also a potent p53 activator .
    • $33
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  • BAY 1892005
    T777682036352-13-1
    BAY 1892005 is a p53 protein modulator that targets the p53 condenser for the study of diseases associated with misfolded p53 protein
    • $93
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  • Kevetrin hydrochloride
    T318466592-89-0
    Kevetrin hydrochloride (4-Isothioureidobutyronitrile hydrochloride) is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
    • $38
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  • NSC348884
    T690981624-55-7
    NSC348884 is a nucleophosmin inhibitor disrupts oligomer formation and induces apoptosis, inhibits cell proliferation at an IC50 of 1.7-4.0 μM in distinct cancer cell lines.
    • $35
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  • Serdemetan
    T2243881202-45-5
    Serdemetan (JNJ-26854165) is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
    • $39
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  • Indole-3-carbinol
    T2947700-06-1
    Indole-3-carbinol (I3C), a naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, inhibits NF-κB and IκBα kinase activation.
    • $29
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  • NSC59984
    T6910803647-40-7
    NSC59984, a p53 pathway activator, induces mutant p53 protein degradation and p73 activation.
    • $64
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  • MIRA-1
    T2298072835-26-8
    MIRA-1 (WRN Helicase Inhibitor) is a restorer of wild-type p53 conformation/cellular function and selectively inhibits Werner syndrome WRN helicase activity with an IC50 of 20 µM.
    • $34
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  • Amifostine thiol
    T3753831098-42-7
    Amifostine thiol (WR-1065) is a radioprotectant that protects DNA from fast neutron-induced strand breaks.Amifostine thiol ameliorates (P<0.001) 6-OHDA-induced stiffness in a dose-dependent manner and activates p53 through a JNK-dependent signaling pathway.
    • $30
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  • 1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one
    TN5263569-83-5
    1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one (Xanthohumol) , prenylchacone flavonoid, is a natural product with multi-biofunctions purified from Hops Humulus lupulus,is effective against HIV-1 and might serve as an interesting lead compound. It may represent a novel chemotherapeutic agent for HIV-1 infection.
    • $36
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  • Tenovin-1
    T1919380315-80-0
    Tenovin-1 inhibits protein-deacetylating activities of SirT1 and SirT2 and protects against MDM2-mediated p53 degradation, which involves ubiquitination.
    • $50
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  • Roslin 2 bromide
    T2473029574-21-8In house
    Roslin 2 bromide (Benzylhexamethylenetetramine bromide) is a p53 reactivator that disrupts the binding of FAK and p5, exhibiting anticancer effects.
    • $44
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  • RO8994
    T35171309684-94-3
    RO8994 is a highly effective and specific inhibitor of spiroindolinone small-molecule MDM2, with IC50 of 20 nM (MTT proliferation assays) and 5 nM (HTRF binding assays).
    • $29
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  • P53R3
    T41068922150-12-7In house
    P53R3 is a potent reactivator of p53, effectively restoring sequence-specific DNA binding to several p53 hot spot mutants, namely p53 R175H, p53 R248W, and p53 R273H. This compound exhibits p53-dependent antiproliferative effects with significantly higher specificity compared to PRIMA-1 and promotes the recruitment of both wild-type p53 and p53 M237I to various target gene promoters. Additionally, P53R3 markedly increases the mRNA, total protein, and cell surface expression of death receptor 5 (DR5), demonstrating its utility in cancer research.
    • $68
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  • SCH529074
    T37042922150-11-6
    SCH529074 is a selective activator of p53 (Ki = 1 μM) and can be used in studies about non-small-cell lung carcinoma. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53.
    • $30
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  • COTI-2
    T43251039455-84-9
    COTI-2, an orally available thiosemicarbazone, is an activator of mutant forms of the p53 protein with potential antineoplastic activity.
    • $38
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  • DPBQ
    T110927029-89-2In house
    DPBQ (ZINC1620467) is a p53 activator. DPBQ could activate p53 and trigger apoptosis in a polyploid-specific manner, without inhibition of topoisomerase or bind DNA.
    • $107
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  • p53-Mdm2 inhibitor 4
    T67698350678-63-6
    p53-Mdm2 inhibitor 4 inhibits the p53-MDM2 protein-protein interaction.
    • $30
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  • CT-1
    T270931983924-33-9In house
    CT-1 is a DNA minor groove ligand and causes p53-dependent breast cancer cell apoptosis.
    • $117
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  • ReACp53 acetate
    TP1427L
    ReACp53 acetate could inhibit p53 amyloid formation and rescue p53 function in cancer cell lines.
    • $55
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  • PK11007
    T7703874146-69-7
    PK11007 is an anti-p53 drug.
    • $32
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  • CP-31398 dihydrochloride
    T216481217195-61-3
    CP-31398 dihydrochloride is a p53 stabilizer which stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53.
    • $42
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  • Ergosta-4,6,8(14),22-tetraen-3-one
    TN161719254-69-4
    Ergosta-4,6,8(14),22-tetraen-3-one exhibits cytotoxic activity against human gastric cancer cells and can induce G2 M cell cycle arrest and apoptosis in human hepatocellular carcinoma (HepG2) cells. These findings could facilitate the further use of various medicinal fungi in cancer treatment.
    • $317
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