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). |
-
J Exp Clin Cancer Res, 2022, 41(1):130
-
Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00063-7
-
PLoS Pathog, 2022, 18(3):e1010365
|
|
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. |
-
Chin Med J (Engl), 2022, 135(5):606-618
-
Shock, 2021, 55(1):74-82
-
Radiat Res, 2020, 193(2):119-129
|
|
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. |
-
Phytomedicine, 2022, 98:153963
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Nat Commun, 2021, 12(1):4019
|
|
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. |
-
Adv Sci (Weinh), 2022, e2200742
-
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
-
Redox Biol, 2022, 50:102240
|
|
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. |
-
Signal Transduct Target Ther, 2022, 7(1):97
-
iScience, 2021, 24(9):103080
-
Cancer Res, 2020, canres.3499.2019
|
|
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. |
-
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Hum Cell, 2021, 10.1007/s13577-021-00639-4
|
|
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. |
-
Cells, 2022, 11(5)794
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Haematologica, 2021, 10.3324/haematol.2020.259531
|
|
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). |
- J Exp Clin Cancer Res, 2022, 41(1):130
- Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00063-7
- PLoS Pathog, 2022, 18(3):e1010365
|
|
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. |
- Chin Med J (Engl), 2022, 135(5):606-618
- Shock, 2021, 55(1):74-82
- Radiat Res, 2020, 193(2):119-129
|
|
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. |
- Phytomedicine, 2022, 98:153963
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Nat Commun, 2021, 12(1):4019
|
|
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. |
- Adv Sci (Weinh), 2022, e2200742
- Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
- Redox Biol, 2022, 50:102240
|
|
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. |
|
|
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. |
- Signal Transduct Target Ther, 2022, 7(1):97
- iScience, 2021, 24(9):103080
- Cancer Res, 2020, canres.3499.2019
|
|
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. |
- Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Hum Cell, 2021, 10.1007/s13577-021-00639-4
|
|
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. |
- Cells, 2022, 11(5)794
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Haematologica, 2021, 10.3324/haematol.2020.259531
|
|
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
|
|