p53

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p53 Signaling Pathway Map

p53 Signaling Pathways

p53 Products

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  • p53 Inhibitors (7)
  • p53 Antibodie (1)
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  • p53 Modulators (2)
  • New p53 Products
Catalog No. Product Name Information Product Use Citations Product Validations
S2929 Pifithrin-α (PFTα) HBr Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes. Pifithrin-α is also a potent agonist of the aryl hydrocarbon receptor (AhR).
Br J Pharmacol, 2021, 10.1111/bph.15385
Development, 2021, dev.188276
Biochim Biophys Acta Mol Cell Res, 2021, 1869(2):119174
S2930 Pifithrin-μ Pifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.
Shock, 2021, 55(1):74-82
Radiat Res, 2020, 193(2):119-129
Clin Transl Med, 2020, 10.1002/ctm2.41
S5791 Cyclic Pifithrin-α hydrobromide Cyclic Pifithrin-α hydrobromide is the hydrobromide salt form of Cyclic Pifithrin-α, which is a transcriptional inhibitor of p53.
Clin Transl Med, 2020, 10.1002/ctm2.41
S7030 RG-7112 RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.
Nat Commun, 2021, 12(1):4019
Cells, 2021, 10(4)742
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S8059 Nutlin-3a Nutlin-3a ((-)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay. Nutlin-3a induces autophagy and apoptosis in a p53-dependent manner.
PLoS Biol, 2021, 19(8):e3001364
Cell Death Dis, 2021, 12(7):663
Cell Death Dis, 2021, 12(4):364
S8187 ReACp53 ReACp53 is a cell-penetrating peptide, designed to inhibit p53 amyloid formation, resues p53 function in cancer cell lines and in organoids derived from high-grade serous ovarian carcinomas (HGSOC).
S9235 Didymin Didymin (Neoponcirin, Isosakuranetin-7-O-rutinoside) is a citrus-derived natural compound that kills p53 wild-type as well as drug-resistant p53-mutant neuroblastoma cells in culture. It possesses antioxidant, anti-inflammation and anti-cancer properties.
A5182 p63 Rabbit Recombinant mAb p63 Rabbit Recombinant mAb detects endogenous level of total p63.
S0507 CBL0137 CBL0137 (Curaxin-137) is an inhibitor of the histone chaperone FACT (facilitates chromatin transcription) that simultaneously suppresses NF-κB and activates p53 with EC50 of 0.47 μM and 0.37 μM, respectively.
Cancer Lett, 2021, 520:201-212
Cancer Lett, 2021, 499:232-242
PLoS One, 2021, 16(6):e0252504
S1172 Serdemetan (JNJ-26854165) Serdemetan (JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53. Phase 1.
iScience, 2021, 24(9):103080
Cancer Res, 2020, canres.3499.2019
Circulation, 2020, 10.1161/CIRCULATIONAHA.120.048191
S2176 Tenovin-3 Tenovin-3 is an inhibitor of SIRT2. Tenovin-3 is able to increase p53 levels in MCF-7 cells.
S2341 (-)-Parthenolide (-)-Parthenolide, an inhibitor of the Nuclear Factor-κB Pathway, specifically depletes HDAC1 protein without affecting other class I/II HDACs; Also promotes the ubiquitination of MDM2 and activates p53 cellular functions.
PLoS Genet, 2021, 17(11):e1009890
Theranostics, 2020, 10(22):9923-9936
J Biol Chem, 2020, 295(11):3576-3589
S2427 Triglycidyl Isocyanurate (Teroxirone) Triglycidyl Isocyanurate (Teroxirone, Tris(2,3-epoxypropyl) Isocyanurate, TGI, TGIC) is a triazene triepoxide with antineoplastic activity. It inhibits growth of human non-small cell lung cancer cells by activating p53. Triglycidyl Isocyanurate alkylates and cross-links DNA, thereby inhibiting DNA replication. Triglycidyl Isocyanurate is also used in various polyester powder coatings in the metal finishing industry.
S2678 NSC 207895 NSC 207895 (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.
Genes Dev, 2020, 34(7-8):526-543
Oncotarget, 2020, 11(46):4224-4242
Sci Rep, 2019, 9(1):1897
S2781 RITA (NSC 652287) RITA (NSC 652287) induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks, and also inhibits MDM2-p53 interaction by targeting p53.
Cancer Cell, 2020, S1535-6108(20)30605-X
Cancers (Basel), 2020, 12(9)E2668
Cancer Discov, 2020, CD-20-0160
S4900 Tenovin-6 Tenovin-6 is a small molecule activator of p53 transcriptional activity and inhibits dihydroorotate dehydrogenase (DHODH). Tenovin-6 is also an inhibitor of SirT1 and SirT2.
Front Immunol, 2021, 12:685523
Biomed Pharmacother, 2020, 125:109948
J Cell Sci, 2019, 132(6)
S5811 Kevetrin hydrochloride Kevetrin hydrochloride (Thioureidobutyronitrile) is a water-soluble, small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
S7149 NSC 319726 NSC319726 is a p53(R175) mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, with IC50 of 8 nM for p53(R175) mutant, shows no inhibition for p53 wild-type cells.
Microbiol Spectr, 2021, 9(3):e0139521
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
S7649 MI-773 (SAR405838) MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
Cell Rep, 2021, 36(5):109482
NPJ Precis Oncol, 2021, 5(1):96
Cancers (Basel), 2020, 12(8):E2157
S7723 PRIMA-1 PRIMA-1 (2,2-Bis(hydroxymethyl)-3-quinuclidinone) is a mutant p53 reactivator. It induces apoptosis and inhibits growth of human tumors with mutant p53.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S7724 Eprenetapopt (APR-246) Eprenetapopt (APR-246, PRIMA-1MET) is a small organic molecule that has been shown to restore tumour-suppressor function primarily to mutant p53 and also to induce cell death in various cancer types. APR-246 induces apoptosis and autophagy.
Haematologica, 2021, 10.3324/haematol.2020.259531
Cancers (Basel), 2021, 13(17)4476
Int J Mol Sci, 2021, 22(11)5782
S8000 Tenovin-1 Tenovin-1 protects against MDM2-mediated p53 degradation, which involves ubiquitination, and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also an inhibitor of dihydroorotate dehydrogenase (DHODH).
J Pharm Biomed Anal, 2021, 201:114121
J Transl Med, 2019, 17(1):76
Sci Rep, 2019, 9(1):1897
S8106 NSC59984 NSC59984 is a p53 pathway activator via induction of mutant p53 protein degradation and p73 activation.
Front Bioeng Biotechnol, 2020, 8:538663
Micromachines (Basel), 2020, 11(2)
S8149 NSC348884 NSC348884, as a nucleophosmin inhibitor, inhibit cell proliferation and induce apoptosis in various cancer cell lines with IC50 values ranging from 1.4-4 µM.
Nat Commun, 2020, 3;11(1):1669
Virulence, 2020, 11(1):1379-1393
Reproduction, 2020, 160(4):491-500
S8483 CBL0137 HCl CBL0137 (CBLC137, Curaxin 137) HCl activates p53 and inhibits NF-kB with EC50s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It also inhibits histone chaperone FACT (facilitates chromatin transcription complex).
Cancer Lett, 2021, 520:201-212
Cancer Lett, 2021, 499:232-242
bioRxiv, 2021, 10.1101/2021.04.20.440573
S8580 COTI-2 COTI-2 is an orally available third generation thiosemicarbazone and activator of mutant forms of the p53 protein, with potential antineoplastic activity.
DASH, 2020, None
S6851 RA-190 RA190, a bis-benzylidine piperidon, is a potent, selective and oral effective inhibitor of proteasome ubiquitin receptor RPN13/ADRM1 with anticancer activity. RA190 triggers ER stress response, p53/p21 signaling axis and autophagy in multiple myeloma cells.
S6882 HI-TOPK-032 HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells.
E0035New CP-31398 Dihydrochloride

CP-31398 Dihydrochloride stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53.

S8728 PK11000 PK11000 stabilizes the DBD of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding and effective in inducing cell death.
S2929 Pifithrin-α (PFTα) HBr Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes. Pifithrin-α is also a potent agonist of the aryl hydrocarbon receptor (AhR).
Br J Pharmacol, 2021, 10.1111/bph.15385
Development, 2021, dev.188276
Biochim Biophys Acta Mol Cell Res, 2021, 1869(2):119174
S2930 Pifithrin-μ Pifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.
Shock, 2021, 55(1):74-82
Radiat Res, 2020, 193(2):119-129
Clin Transl Med, 2020, 10.1002/ctm2.41
S5791 Cyclic Pifithrin-α hydrobromide Cyclic Pifithrin-α hydrobromide is the hydrobromide salt form of Cyclic Pifithrin-α, which is a transcriptional inhibitor of p53.
Clin Transl Med, 2020, 10.1002/ctm2.41
S7030 RG-7112 RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.
Nat Commun, 2021, 12(1):4019
Cells, 2021, 10(4)742
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S8059 Nutlin-3a Nutlin-3a ((-)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay. Nutlin-3a induces autophagy and apoptosis in a p53-dependent manner.
PLoS Biol, 2021, 19(8):e3001364
Cell Death Dis, 2021, 12(7):663
Cell Death Dis, 2021, 12(4):364
S8187 ReACp53 ReACp53 is a cell-penetrating peptide, designed to inhibit p53 amyloid formation, resues p53 function in cancer cell lines and in organoids derived from high-grade serous ovarian carcinomas (HGSOC).
S9235 Didymin Didymin (Neoponcirin, Isosakuranetin-7-O-rutinoside) is a citrus-derived natural compound that kills p53 wild-type as well as drug-resistant p53-mutant neuroblastoma cells in culture. It possesses antioxidant, anti-inflammation and anti-cancer properties.
A5182 p63 Rabbit Recombinant mAb p63 Rabbit Recombinant mAb detects endogenous level of total p63.
S0507 CBL0137 CBL0137 (Curaxin-137) is an inhibitor of the histone chaperone FACT (facilitates chromatin transcription) that simultaneously suppresses NF-κB and activates p53 with EC50 of 0.47 μM and 0.37 μM, respectively.
Cancer Lett, 2021, 520:201-212
Cancer Lett, 2021, 499:232-242
PLoS One, 2021, 16(6):e0252504
S1172 Serdemetan (JNJ-26854165) Serdemetan (JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53. Phase 1.
iScience, 2021, 24(9):103080
Cancer Res, 2020, canres.3499.2019
Circulation, 2020, 10.1161/CIRCULATIONAHA.120.048191
S2176 Tenovin-3 Tenovin-3 is an inhibitor of SIRT2. Tenovin-3 is able to increase p53 levels in MCF-7 cells.
S2341 (-)-Parthenolide (-)-Parthenolide, an inhibitor of the Nuclear Factor-κB Pathway, specifically depletes HDAC1 protein without affecting other class I/II HDACs; Also promotes the ubiquitination of MDM2 and activates p53 cellular functions.
PLoS Genet, 2021, 17(11):e1009890
Theranostics, 2020, 10(22):9923-9936
J Biol Chem, 2020, 295(11):3576-3589
S2427 Triglycidyl Isocyanurate (Teroxirone) Triglycidyl Isocyanurate (Teroxirone, Tris(2,3-epoxypropyl) Isocyanurate, TGI, TGIC) is a triazene triepoxide with antineoplastic activity. It inhibits growth of human non-small cell lung cancer cells by activating p53. Triglycidyl Isocyanurate alkylates and cross-links DNA, thereby inhibiting DNA replication. Triglycidyl Isocyanurate is also used in various polyester powder coatings in the metal finishing industry.
S2678 NSC 207895 NSC 207895 (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.
Genes Dev, 2020, 34(7-8):526-543
Oncotarget, 2020, 11(46):4224-4242
Sci Rep, 2019, 9(1):1897
S2781 RITA (NSC 652287) RITA (NSC 652287) induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks, and also inhibits MDM2-p53 interaction by targeting p53.
Cancer Cell, 2020, S1535-6108(20)30605-X
Cancers (Basel), 2020, 12(9)E2668
Cancer Discov, 2020, CD-20-0160
S4900 Tenovin-6 Tenovin-6 is a small molecule activator of p53 transcriptional activity and inhibits dihydroorotate dehydrogenase (DHODH). Tenovin-6 is also an inhibitor of SirT1 and SirT2.
Front Immunol, 2021, 12:685523
Biomed Pharmacother, 2020, 125:109948
J Cell Sci, 2019, 132(6)
S5811 Kevetrin hydrochloride Kevetrin hydrochloride (Thioureidobutyronitrile) is a water-soluble, small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
S7149 NSC 319726 NSC319726 is a p53(R175) mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, with IC50 of 8 nM for p53(R175) mutant, shows no inhibition for p53 wild-type cells.
Microbiol Spectr, 2021, 9(3):e0139521
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
S7649 MI-773 (SAR405838) MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
Cell Rep, 2021, 36(5):109482
NPJ Precis Oncol, 2021, 5(1):96
Cancers (Basel), 2020, 12(8):E2157
S7723 PRIMA-1 PRIMA-1 (2,2-Bis(hydroxymethyl)-3-quinuclidinone) is a mutant p53 reactivator. It induces apoptosis and inhibits growth of human tumors with mutant p53.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S7724 Eprenetapopt (APR-246) Eprenetapopt (APR-246, PRIMA-1MET) is a small organic molecule that has been shown to restore tumour-suppressor function primarily to mutant p53 and also to induce cell death in various cancer types. APR-246 induces apoptosis and autophagy.
Haematologica, 2021, 10.3324/haematol.2020.259531
Cancers (Basel), 2021, 13(17)4476
Int J Mol Sci, 2021, 22(11)5782
S8000 Tenovin-1 Tenovin-1 protects against MDM2-mediated p53 degradation, which involves ubiquitination, and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also an inhibitor of dihydroorotate dehydrogenase (DHODH).
J Pharm Biomed Anal, 2021, 201:114121
J Transl Med, 2019, 17(1):76
Sci Rep, 2019, 9(1):1897
S8106 NSC59984 NSC59984 is a p53 pathway activator via induction of mutant p53 protein degradation and p73 activation.
Front Bioeng Biotechnol, 2020, 8:538663
Micromachines (Basel), 2020, 11(2)
S8149 NSC348884 NSC348884, as a nucleophosmin inhibitor, inhibit cell proliferation and induce apoptosis in various cancer cell lines with IC50 values ranging from 1.4-4 µM.
Nat Commun, 2020, 3;11(1):1669
Virulence, 2020, 11(1):1379-1393
Reproduction, 2020, 160(4):491-500
S8483 CBL0137 HCl CBL0137 (CBLC137, Curaxin 137) HCl activates p53 and inhibits NF-kB with EC50s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It also inhibits histone chaperone FACT (facilitates chromatin transcription complex).
Cancer Lett, 2021, 520:201-212
Cancer Lett, 2021, 499:232-242
bioRxiv, 2021, 10.1101/2021.04.20.440573
S8580 COTI-2 COTI-2 is an orally available third generation thiosemicarbazone and activator of mutant forms of the p53 protein, with potential antineoplastic activity.
DASH, 2020, None
S6851 RA-190 RA190, a bis-benzylidine piperidon, is a potent, selective and oral effective inhibitor of proteasome ubiquitin receptor RPN13/ADRM1 with anticancer activity. RA190 triggers ER stress response, p53/p21 signaling axis and autophagy in multiple myeloma cells.
S6882 HI-TOPK-032 HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells.
E0035New CP-31398 Dihydrochloride

CP-31398 Dihydrochloride stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53.

Tags: p53 apoptosis | p53 inhibition | p53 cancer | p53 mutation | p53 protein | p53 pathway | p53 activation | p53 phosphorylation | p53 activity | p53-dependent apoptosis | p53 apoptosis pathway | p53 cancer therapy | p53-independent apoptosis | p53-mdm2 interaction | p53-p21 pathway | p53-mdm2 pathway | p53 protein structure | p53 protein function | p53 cleavage | p53 inhibitor review