p53

Signaling Pathway Map

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Inhibitory Selectivity

p53 Products

All (21) p53 Inhibitors (6) p53 Activators (15) New p53 Products

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.	Redox Biol, 2019, 22:101157 Stem Cell Res Ther, 2019, 10(1):123 Cancer Med, 2019, 10.1002/cam4.2393	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.
S5791^New	Cyclic Pifithrin-α hydrobromide Cyclic Pifithrin-α hydrobromide is the hydrobromide salt form of Cyclic Pifithrin-α, which is a transcriptional inhibitor of p53.
S9235^New	Didymin Didymin 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.
S2930	Pifithrin-μ Pifithrin-μ is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.	Front Pharmacol, 2018, 9:92 Oncogene, 2018, 37(8):1041-1048 Int J Mol Med, 2018, 42(4):2089-2097	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.
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.
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.	Cancer Cell, 2019, 36(2):179-193 BMC Pharmacol Toxicol, 2017, 18(1):40 Sci Signal, 2016, 9(448):ra98
S2678	NSC 207895 NSC 207895 suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.	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.	Cancer Cell, 2019, 35(2):191-203 Nat Chem Biol, 2015, 10.1038/nchembio.1986 Oncogene, 2014, 10.1038/onc.2014.37	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.
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.	J Transl Med, 2019, 17(1):76	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.
S5811^New	Kevetrin hydrochloride Kevetrin hydrochloride 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.
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.	Oncotarget, 2016, 7(50):82757-82769	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.	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.
S8106	NSC59984 NSC59984 is a p53 pathway activator via induction of mutant p53 protein degradation and p73 activation.
S8483	CBL0137 (CBL-0137) CBL0137(CBL-0137) 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).
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.	Biochem Biophys Res Commun, 2018, 501(1):246-252 Oncol Rep, 2018, 39(3):1181-1190 J Neuroimmunol, 2017, 305:154-161	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	PK11007 PK11007 is an anti-p53 drug that stabilizes wild type and mutant p53 via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity. It exerts antitumor functions not only via reactivating p53 but also via other cellular mechanisms, such as increase of cellular ROS to toxic levels and activation of the UPR.

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.	Redox Biol, 2019, 22:101157 Stem Cell Res Ther, 2019, 10(1):123 Cancer Med, 2019, 10.1002/cam4.2393	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.
S5791^New	Cyclic Pifithrin-α hydrobromide Cyclic Pifithrin-α hydrobromide is the hydrobromide salt form of Cyclic Pifithrin-α, which is a transcriptional inhibitor of p53.
S9235^New	Didymin Didymin 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.
S2930	Pifithrin-μ Pifithrin-μ is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.	Front Pharmacol, 2018, 9:92 Oncogene, 2018, 37(8):1041-1048 Int J Mol Med, 2018, 42(4):2089-2097	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.
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.
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.	Cancer Cell, 2019, 36(2):179-193 BMC Pharmacol Toxicol, 2017, 18(1):40 Sci Signal, 2016, 9(448):ra98
S2678	NSC 207895 NSC 207895 suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.	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.	Cancer Cell, 2019, 35(2):191-203 Nat Chem Biol, 2015, 10.1038/nchembio.1986 Oncogene, 2014, 10.1038/onc.2014.37	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.
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.	J Transl Med, 2019, 17(1):76	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.
S5811^New	Kevetrin hydrochloride Kevetrin hydrochloride 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.
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.	Oncotarget, 2016, 7(50):82757-82769	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.	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.
S8106	NSC59984 NSC59984 is a p53 pathway activator via induction of mutant p53 protein degradation and p73 activation.
S8483	CBL0137 (CBL-0137) CBL0137(CBL-0137) 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).
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.	Biochem Biophys Res Commun, 2018, 501(1):246-252 Oncol Rep, 2018, 39(3):1181-1190 J Neuroimmunol, 2017, 305:154-161	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	PK11007 PK11007 is an anti-p53 drug that stabilizes wild type and mutant p53 via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity. It exerts antitumor functions not only via reactivating p53 but also via other cellular mechanisms, such as increase of cellular ROS to toxic levels and activation of the UPR.

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p53

Signaling Pathway Map

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Inhibitory Selectivity

p53 Products