p53

p53製品

• All (36)
• p53阻害剤 (12)
• p53活性剤(20)
• p53モジュレータ(2)
• 新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
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).	Cell Death Differ, 2024, 31(8):999-1012 Int J Biol Sci, 2024, 20(6):2008-2026 Cell Mol Life Sci, 2024, 81(1):101
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.	EMBO J, 2024, 10.1038/s44318-024-00240-z J Neuroinflammation, 2024, 21(1):57 Front Immunol, 2024, 15:1374943
S7030	RG-7112	RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.	Int J Mol Sci, 2024, 25(7)3948 bioRxiv, 2024, 2024.10.09.617493 Biomolecules, 2023, 13(8)1257
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.	Cell Mol Life Sci, 2024, 81(1):384 iScience, 2023, 26(7):107090 Heliyon, 2023, 9(3):e14169
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.	Genes Environ, 2024, 46(1):10 Transl Oncol, 2023, 35:101712 PLoS Genet, 2021, 17(11):e1009890
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.	Oncotarget, 2024, 15:614-633 J Cell Mol Med, 2024, 28(9):e18374 Cell Death Dis, 2023, 14(11):783
S7649	MI-773 (SAR405838)	MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.	Pharmaceutics, 2023, 15(4)1274 Haematologica, 2022, 10.3324/haematol.2022.280879 Oncogenesis, 2022, 11(1):37
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.	Signal Transduct Target Ther, 2022, 7(1):97 iScience, 2021, 24(9):103080 Circulation, 2020, 10.1161/CIRCULATIONAHA.120.048191
S2781	RITA	RITA 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.	Cell Death Discov, 2024, 10(1):381 J Cancer, 2023, 14(2):200-218 Theranostics, 2022, 12(9):4110-4126
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.	PLoS One, 2024, 19(1):e0295629 Front Oncol, 2021, 11:582511 Genes Dev, 2020, 34(7-8):526-543
S8483	CBL0137 HCl	CBL0137 (CBLC137, Curaxin 137) HCl activates p53 and inhibits NF-κB 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).	JCI Insight, 2023, 8(4)e154120 J Exp Clin Cancer Res, 2022, 41(1):355 Cancer Lett, 2021, 520:201-212
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 Med, 2024, 13(20):e70288 JCI Insight, 2023, 8(4)e154120 Biomed Pharmacother, 2023, 161:114529
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.	J Control Release, 2024, 371:111-125 Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 J Pers Med, 2022, 12(2)258
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 Int J Mol Med, 2019, 44(3):1091-1105
S7149	NSC 319726 (ZMC1)	NSC 319726 (ZMC1) 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
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.	Cell Death Dis, 2023, 14(10):667 Front Immunol, 2021, 12:685523 Biomed Pharmacother, 2020, 125:109948
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.	Front Immunol, 2022, 13:956991 Nat Commun, 2020, 3;11(1):1669 Virulence, 2020, 11(1):1379-1393
S8106	NSC59984	NSC59984 is a p53 pathway activator via induction of mutant p53 protein degradation and p73 activation.	Cancers (Basel), 2023, 15(3)745 J Clin Med, 2023, 12(23)7491 Front Bioeng Biotechnol, 2020, 8:538663
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.	Front Pharmacol, 2022, 13:926317 Clin Transl Med, 2020, 10.1002/ctm2.41
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.	J Cell Mol Med, 2024, 28(9):e18374 DASH, 2020, None
S5811	Kevetrin hydrochloride	Kevetrin hydrochloride (Thioureidobutyronitrile) is a water-soluble, small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.	Int J Mol Sci, 2022, 23(17)10042
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).	PNAS Nexus, 2022, 1(3):pgac128 Nat Commun, 2021, 12(1):3962
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.
E1971New	Rezatapopt	Rezatapopt(PC14586) is a first-in-class p53 reactivator. It selectively binds to the mutated p53 Y220C protein and restores its wild-type activity. It can also be used to inhibit solid tumor with p53 mutation.
S2176	Tenovin-3	Tenovin-3 is an inhibitor of SIRT2. Tenovin-3 is able to increase p53 levels in MCF-7 cells.
E0935	MS7972	MS7972 is a small molecule that blocks human p53 and CREB binding protein association.
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.
E0068	NiCur	NiCur is a small molecule which blocks CREB-binding protein (CBP) histone acetyltransferase (HAT) activity and downregulates p53 activation upon genotoxic stress and diminishs the recruitment of p53 as well as RNA Polymerase II and levels of acetylation on histone H3 on CDKN1A promoter.
E0394	YK 3-237	YK-3-237, a SIRT1 activator, reduces acetylation of mutant p53 and inhibits the proliferation of triple-negative breast cancer cells.
E2943	Pifithrin-β	Pifithrin-β (PFT β hydrobromide; Cyclic Pifithrin-α hydrobromide) is a potent inhibitor of p53 with an IC50 of 23 μM and is regarded as a lead compound for cancer and neurodegenerative disease therapy.
E0035	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.
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.
E1735	PK11007	PK11007 is a thiol-reactive anticancer agent that stabilizes p53 via selective alkylation of two surface cysteines without compromising its DNA binding. It induces mutant p53 cancer cell death by increasing reactive oxygen species (ROS) levels.
S9488New	Lobetyolin	Lobetyolin is one of the important active ingredients extracted from the root of Codonopsis pilosula, which has a good protective effect on gastric mucosal damage. Lobetyolin can downregulate glutamine metabolism, contribute to drug-induced apoptosis and tumor growth inhibition, and lobetyolin significantly reduces the mRNA and protein expression of the amino acid transporter alanine-serine-cysteine ​​transporter 2 (ASCT2).
S8728	PK11000	PK11000 stabilizes the DBD of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding and is effective in inducing cell death.
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.
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).	Cell Death Differ, 2024, 31(8):999-1012 Int J Biol Sci, 2024, 20(6):2008-2026 Cell Mol Life Sci, 2024, 81(1):101
S7030	RG-7112	RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.	Int J Mol Sci, 2024, 25(7)3948 bioRxiv, 2024, 2024.10.09.617493 Biomolecules, 2023, 13(8)1257
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.	Cell Mol Life Sci, 2024, 81(1):384 iScience, 2023, 26(7):107090 Heliyon, 2023, 9(3):e14169
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.	Front Pharmacol, 2022, 13:926317 Clin Transl Med, 2020, 10.1002/ctm2.41
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).	PNAS Nexus, 2022, 1(3):pgac128 Nat Commun, 2021, 12(1):3962
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.
E0935	MS7972	MS7972 is a small molecule that blocks human p53 and CREB binding protein association.
E0068	NiCur	NiCur is a small molecule which blocks CREB-binding protein (CBP) histone acetyltransferase (HAT) activity and downregulates p53 activation upon genotoxic stress and diminishs the recruitment of p53 as well as RNA Polymerase II and levels of acetylation on histone H3 on CDKN1A promoter.
E0394	YK 3-237	YK-3-237, a SIRT1 activator, reduces acetylation of mutant p53 and inhibits the proliferation of triple-negative breast cancer cells.
E2943	Pifithrin-β	Pifithrin-β (PFT β hydrobromide; Cyclic Pifithrin-α hydrobromide) is a potent inhibitor of p53 with an IC50 of 23 μM and is regarded as a lead compound for cancer and neurodegenerative disease therapy.
E1735	PK11007	PK11007 is a thiol-reactive anticancer agent that stabilizes p53 via selective alkylation of two surface cysteines without compromising its DNA binding. It induces mutant p53 cancer cell death by increasing reactive oxygen species (ROS) levels.
S9488New	Lobetyolin	Lobetyolin is one of the important active ingredients extracted from the root of Codonopsis pilosula, which has a good protective effect on gastric mucosal damage. Lobetyolin can downregulate glutamine metabolism, contribute to drug-induced apoptosis and tumor growth inhibition, and lobetyolin significantly reduces the mRNA and protein expression of the amino acid transporter alanine-serine-cysteine ​​transporter 2 (ASCT2).
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.	EMBO J, 2024, 10.1038/s44318-024-00240-z J Neuroinflammation, 2024, 21(1):57 Front Immunol, 2024, 15:1374943
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.	Genes Environ, 2024, 46(1):10 Transl Oncol, 2023, 35:101712 PLoS Genet, 2021, 17(11):e1009890
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.	Oncotarget, 2024, 15:614-633 J Cell Mol Med, 2024, 28(9):e18374 Cell Death Dis, 2023, 14(11):783
S7649	MI-773 (SAR405838)	MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.	Pharmaceutics, 2023, 15(4)1274 Haematologica, 2022, 10.3324/haematol.2022.280879 Oncogenesis, 2022, 11(1):37
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.	Signal Transduct Target Ther, 2022, 7(1):97 iScience, 2021, 24(9):103080 Circulation, 2020, 10.1161/CIRCULATIONAHA.120.048191
S2781	RITA	RITA 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.	Cell Death Discov, 2024, 10(1):381 J Cancer, 2023, 14(2):200-218 Theranostics, 2022, 12(9):4110-4126
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.	PLoS One, 2024, 19(1):e0295629 Front Oncol, 2021, 11:582511 Genes Dev, 2020, 34(7-8):526-543
S8483	CBL0137 HCl	CBL0137 (CBLC137, Curaxin 137) HCl activates p53 and inhibits NF-κB 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).	JCI Insight, 2023, 8(4)e154120 J Exp Clin Cancer Res, 2022, 41(1):355 Cancer Lett, 2021, 520:201-212
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 Med, 2024, 13(20):e70288 JCI Insight, 2023, 8(4)e154120 Biomed Pharmacother, 2023, 161:114529
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.	J Control Release, 2024, 371:111-125 Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 J Pers Med, 2022, 12(2)258
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 Int J Mol Med, 2019, 44(3):1091-1105
S7149	NSC 319726 (ZMC1)	NSC 319726 (ZMC1) 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
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.	Cell Death Dis, 2023, 14(10):667 Front Immunol, 2021, 12:685523 Biomed Pharmacother, 2020, 125:109948
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.	Front Immunol, 2022, 13:956991 Nat Commun, 2020, 3;11(1):1669 Virulence, 2020, 11(1):1379-1393
S8106	NSC59984	NSC59984 is a p53 pathway activator via induction of mutant p53 protein degradation and p73 activation.	Cancers (Basel), 2023, 15(3)745 J Clin Med, 2023, 12(23)7491 Front Bioeng Biotechnol, 2020, 8:538663
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.	J Cell Mol Med, 2024, 28(9):e18374 DASH, 2020, None
S5811	Kevetrin hydrochloride	Kevetrin hydrochloride (Thioureidobutyronitrile) is a water-soluble, small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.	Int J Mol Sci, 2022, 23(17)10042
E1971New	Rezatapopt	Rezatapopt(PC14586) is a first-in-class p53 reactivator. It selectively binds to the mutated p53 Y220C protein and restores its wild-type activity. It can also be used to inhibit solid tumor with p53 mutation.
S2176	Tenovin-3	Tenovin-3 is an inhibitor of SIRT2. Tenovin-3 is able to increase p53 levels in MCF-7 cells.
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.
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.
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.
E1971New	Rezatapopt	Rezatapopt(PC14586) is a first-in-class p53 reactivator. It selectively binds to the mutated p53 Y220C protein and restores its wild-type activity. It can also be used to inhibit solid tumor with p53 mutation.
S9488New	Lobetyolin	Lobetyolin is one of the important active ingredients extracted from the root of Codonopsis pilosula, which has a good protective effect on gastric mucosal damage. Lobetyolin can downregulate glutamine metabolism, contribute to drug-induced apoptosis and tumor growth inhibition, and lobetyolin significantly reduces the mRNA and protein expression of the amino acid transporter alanine-serine-cysteine ​​transporter 2 (ASCT2).

p53シグナル伝達経路