p53

Signaling Pathway Map

Research Area

Inhibitory Selectivity

p53 Products

All (28) p53 Inhibitors (12) p53 Activators (15)

Catalog No.	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).	Neuro Oncol, 2020, noaa207 Cancers (Basel), 2020, 20;12(2) pii: E493 Aging (Albany NY), 2020, 12(18):18649-18659	A, HAECs were per-incubated with PFTα (3 μmol/L) for 60 min followed by transfected with siB-myb or siNC in the presence of PFTα (3 μmol/L) for 7 d. The expression levels of B-myb, p-p53, p53 and p21 proteins were analysed by western blotting. GAPDH was used as a loading control. A typical group of blots is shown from one of three independent experiments.
S8059	Nutlin-3a Nutlin-3a, 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.	Sci Adv, 2020, 6(27):eaaz9072 Oncogenesis, 2020, 1;9(5):57 Cell Discov, 2020, 21;6:21	Nutlin-3a preserved p53 expression without influencing high glucose (HG)-induced podocyte impairment. A-D: cultured podocytes were pre-treated by nutlin-3a for 2 hrs before subjected to HG treatment. Western blotting gel documents (A) and summarized data (B) showing the expression of p53 and MDM2 in podocytes under HG exposure for 24 hrs. n = 4. Western blotting gel documents (C) and summarized data (D) showing the expression of Desmin in podocytes under HG exposure for 24 hrs. n = 3. *P < 0.05 vs. Ctrl, #P < 0.05 vs. Vehl + HG. Ctrl: control; Vehl: vehicle; nutlin-3a: nutlin-3a treatment.
S6882^New	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.
S6851^New	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.
S2176^New	Tenovin-3 Tenovin-3 is an inhibitor of SIRT2. Tenovin-3 is able to increase p53 levels in MCF-7 cells.
S0507^New	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.	Cells, 2020, 9(6):1423
S2930	Pifithrin-μ Pifithrin-μ (NSC 303580, PFTμ) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.	Radiat Res, 2020, 193(2):119-129 Clin Transl Med, 2020, 10.1002/ctm2.41 Theranostics, 2019, 9(2):554-572	Effect of pifithrin-μ (the inhibitor of mitochondrial translocation of p53) on MEG3-induced apoptosis in TGF-β1-treated LX-2 cells. The inhibitor pifithrin-μ attenuated cleavage of caspase 3 which blocked apoptosis. The results are expressed as relative expression against control expression without treatment.
S7030	RG-7112 RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.	Eur J Cancer, 2020, 126:93-103 Elife, 2020, 9:e54693 Nat Commun, 2019, 10(1):2189
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.
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
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 Cell Death Dis, 2019, 10(11):831
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).
S1172	JNJ-26854165 (Serdemetan) JNJ-26854165 (Serdemetan) 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.	Circulation, 2020, 10.1161/CIRCULATIONAHA.120.048191 Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193
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 Oncol Lett, 2018, 15(2):1673-1679 Stem Cell Reports, 2016, 7(6):1140-1151	Median overall survival of mice (n = 5 mice in vehicle and PYR-41; n = 4 mice in NSC group) inoculated with IOWA-1T xenografts were increased to 43 ± 0.5 and 39 ± 2 days with PYR-41 (PYR) and NSC-207895 (NSC), respectively, compared with a vehicle-treated control group 33 ± 1 days (*p < 0.05).
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.	Cancers (Basel), 2020, 12(9)E2668 Cancer Discov, 2020, CD-20-0160 Cancer Cell, 2019, 35(2):191-203	To determine the number of viable cells, cells were serum starved for 8 hours and treated with 25 nM RITA and stimulated with 1ug/mL SDF1α for 48 hours in serum-free media. After 48 hours, cells were harvested and counted by trypan blue exclusion, using standard methods.
S2427^New	Triglycidyl Isocyanurate (Teroxirone) Triglycidyl Isocyanurate, also known as Teroxirone, 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.
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 Transl Med, 2019, 17(1):76 Int J Mol Med, 2019, 44(3):1091-1105	The SIRT1 inhibitor (tenovin-1) partially blocked the protective effect of γ-man in L02 cells. The effect of tenovin-1 on expression and acetylation level of PGC-1α (B) in L02 cells treated with or without γ-man.
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.	Cell, 2020, 182(3):685-712.e19 Cell Chem Biol, 2018, 25(5):585-594
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.
S7649	MI-773 (SAR405838) MI-773 (SAR405838) is an orally available MDM2 antagonist with K_i of 0.88 nM. Phase 1.	Cancers (Basel), 2020, 12(8):E2157 EMBO J, 2019, 38(20):e102096 Cell Chem Biol, 2018, 25(6):761-774	A panel of four NB cell lines were seeded in six-well plates with indicated concentrations of SAR405838 and agar, and grown for 2 to 3 weeks. Cells were stained with crystal violet for 4 hours. Colonies were counted and colony numbers were represented as % vehicle ± S.D. with P < 0.05 (), P < 0.01 () or P < 0.001 (**) (Student's t-test, two-tailed) as indicated.
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.	Biomed Pharmacother, 2020, 125:109948 J Cell Sci, 2019, 132(6) Nat Biotechnol, 2015, 10.1038/nbt.3130
S7724	APR-246 (PRIMA-1MET) APR-246, also known as 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.	BMC Cancer, 2020, 20(1):617
S5811	Kevetrin hydrochloride Kevetrin hydrochloride is a water-soluble, small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
S8106	NSC59984 NSC59984 is a p53 pathway activator via induction of mutant p53 protein degradation and p73 activation.	Micromachines (Basel), 2020, 11(2)
S8483	CBL0137 HCl (CBL-0137 HCl) CBL0137 (Curaxin 137) 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).	Mol Cell, 2020, S1097-2765(20)30193-3 Cells, 2020, 9(6):1423
S7723	PRIMA-1 PRIMA-1 is a mutant p53 reactivator. It induces apoptosis and inhibits growth of human tumors with mutant p53.
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.	J Biol Chem, 2020, 295(11):3576-3589 G3 (Bethesda), 2020, 4;10(5):1585-1597 Onco Targets Ther, 2020, 13:7447-7458	G. To evaluate effects of IKBKE/TBK1 inhibition on NF-κB signaling in Ewing, TC32 cells were incubated with CYT387 for six hours prior to stimulation with TNF-α (30 ng/mL). IκBα degradation was measured by harvesting TC32 cells thirty minutes after stimulation with TNF-α. TNF-α stimulation resulted in degradation of IκBα, and this effect was attenuated with CYT387 treatment. Parthenolide, an inhibitor of IκBα phosphorylation was used as a positive control. Similar effects of CYT387 activity were seen in HEK-293T cells which also express IKBKΕ. Nuclear extracts were prepared from TC32 cells harvested following forty-five minutes of TNF-α stimulation. Treatment with CYT387 resulted in decreased nuclear localization of NF-κB family proteins RelA/p65 and c-Rel. There was a modest impairment of p50 nuclear localization as compared to parthenolide and DMSO controls and no change in p52 nuclear localization. RelB (not shown) is not expressed in TC32 cells
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.

Catalog No.	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).	Neuro Oncol, 2020, noaa207 Cancers (Basel), 2020, 20;12(2) pii: E493 Aging (Albany NY), 2020, 12(18):18649-18659	A, HAECs were per-incubated with PFTα (3 μmol/L) for 60 min followed by transfected with siB-myb or siNC in the presence of PFTα (3 μmol/L) for 7 d. The expression levels of B-myb, p-p53, p53 and p21 proteins were analysed by western blotting. GAPDH was used as a loading control. A typical group of blots is shown from one of three independent experiments.
S8059	Nutlin-3a Nutlin-3a, 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.	Sci Adv, 2020, 6(27):eaaz9072 Oncogenesis, 2020, 1;9(5):57 Cell Discov, 2020, 21;6:21	Nutlin-3a preserved p53 expression without influencing high glucose (HG)-induced podocyte impairment. A-D: cultured podocytes were pre-treated by nutlin-3a for 2 hrs before subjected to HG treatment. Western blotting gel documents (A) and summarized data (B) showing the expression of p53 and MDM2 in podocytes under HG exposure for 24 hrs. n = 4. Western blotting gel documents (C) and summarized data (D) showing the expression of Desmin in podocytes under HG exposure for 24 hrs. n = 3. *P < 0.05 vs. Ctrl, #P < 0.05 vs. Vehl + HG. Ctrl: control; Vehl: vehicle; nutlin-3a: nutlin-3a treatment.
S6882^New	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.
S6851^New	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.
S2176^New	Tenovin-3 Tenovin-3 is an inhibitor of SIRT2. Tenovin-3 is able to increase p53 levels in MCF-7 cells.
S0507^New	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.	Cells, 2020, 9(6):1423
S2930	Pifithrin-μ Pifithrin-μ (NSC 303580, PFTμ) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.	Radiat Res, 2020, 193(2):119-129 Clin Transl Med, 2020, 10.1002/ctm2.41 Theranostics, 2019, 9(2):554-572	Effect of pifithrin-μ (the inhibitor of mitochondrial translocation of p53) on MEG3-induced apoptosis in TGF-β1-treated LX-2 cells. The inhibitor pifithrin-μ attenuated cleavage of caspase 3 which blocked apoptosis. The results are expressed as relative expression against control expression without treatment.
S7030	RG-7112 RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.	Eur J Cancer, 2020, 126:93-103 Elife, 2020, 9:e54693 Nat Commun, 2019, 10(1):2189
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.
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
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 Cell Death Dis, 2019, 10(11):831
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).

Catalog No.	Information	Product Use Citations	Product Validations
S1172	JNJ-26854165 (Serdemetan) JNJ-26854165 (Serdemetan) 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.	Circulation, 2020, 10.1161/CIRCULATIONAHA.120.048191 Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193
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 Oncol Lett, 2018, 15(2):1673-1679 Stem Cell Reports, 2016, 7(6):1140-1151	Median overall survival of mice (n = 5 mice in vehicle and PYR-41; n = 4 mice in NSC group) inoculated with IOWA-1T xenografts were increased to 43 ± 0.5 and 39 ± 2 days with PYR-41 (PYR) and NSC-207895 (NSC), respectively, compared with a vehicle-treated control group 33 ± 1 days (*p < 0.05).
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.	Cancers (Basel), 2020, 12(9)E2668 Cancer Discov, 2020, CD-20-0160 Cancer Cell, 2019, 35(2):191-203	To determine the number of viable cells, cells were serum starved for 8 hours and treated with 25 nM RITA and stimulated with 1ug/mL SDF1α for 48 hours in serum-free media. After 48 hours, cells were harvested and counted by trypan blue exclusion, using standard methods.
S2427^New	Triglycidyl Isocyanurate (Teroxirone) Triglycidyl Isocyanurate, also known as Teroxirone, 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.
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 Transl Med, 2019, 17(1):76 Int J Mol Med, 2019, 44(3):1091-1105	The SIRT1 inhibitor (tenovin-1) partially blocked the protective effect of γ-man in L02 cells. The effect of tenovin-1 on expression and acetylation level of PGC-1α (B) in L02 cells treated with or without γ-man.
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.	Cell, 2020, 182(3):685-712.e19 Cell Chem Biol, 2018, 25(5):585-594
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.
S7649	MI-773 (SAR405838) MI-773 (SAR405838) is an orally available MDM2 antagonist with K_i of 0.88 nM. Phase 1.	Cancers (Basel), 2020, 12(8):E2157 EMBO J, 2019, 38(20):e102096 Cell Chem Biol, 2018, 25(6):761-774	A panel of four NB cell lines were seeded in six-well plates with indicated concentrations of SAR405838 and agar, and grown for 2 to 3 weeks. Cells were stained with crystal violet for 4 hours. Colonies were counted and colony numbers were represented as % vehicle ± S.D. with P < 0.05 (), P < 0.01 () or P < 0.001 (**) (Student's t-test, two-tailed) as indicated.
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.	Biomed Pharmacother, 2020, 125:109948 J Cell Sci, 2019, 132(6) Nat Biotechnol, 2015, 10.1038/nbt.3130
S7724	APR-246 (PRIMA-1MET) APR-246, also known as 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.	BMC Cancer, 2020, 20(1):617
S5811	Kevetrin hydrochloride Kevetrin hydrochloride is a water-soluble, small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
S8106	NSC59984 NSC59984 is a p53 pathway activator via induction of mutant p53 protein degradation and p73 activation.	Micromachines (Basel), 2020, 11(2)
S8483	CBL0137 HCl (CBL-0137 HCl) CBL0137 (Curaxin 137) 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).	Mol Cell, 2020, S1097-2765(20)30193-3 Cells, 2020, 9(6):1423
S7723	PRIMA-1 PRIMA-1 is a mutant p53 reactivator. It induces apoptosis and inhibits growth of human tumors with mutant p53.
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.	J Biol Chem, 2020, 295(11):3576-3589 G3 (Bethesda), 2020, 4;10(5):1585-1597 Onco Targets Ther, 2020, 13:7447-7458	G. To evaluate effects of IKBKE/TBK1 inhibition on NF-κB signaling in Ewing, TC32 cells were incubated with CYT387 for six hours prior to stimulation with TNF-α (30 ng/mL). IκBα degradation was measured by harvesting TC32 cells thirty minutes after stimulation with TNF-α. TNF-α stimulation resulted in degradation of IκBα, and this effect was attenuated with CYT387 treatment. Parthenolide, an inhibitor of IκBα phosphorylation was used as a positive control. Similar effects of CYT387 activity were seen in HEK-293T cells which also express IKBKΕ. Nuclear extracts were prepared from TC32 cells harvested following forty-five minutes of TNF-α stimulation. Treatment with CYT387 resulted in decreased nuclear localization of NF-κB family proteins RelA/p65 and c-Rel. There was a modest impairment of p50 nuclear localization as compared to parthenolide and DMSO controls and no change in p52 nuclear localization. RelB (not shown) is not expressed in TC32 cells

Catalog No.	Information	Product Use Citations	Product Validations
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.

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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.

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