| S2929 |
Pifithrin-α (PFTα) Hhydrobromide
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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).
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J Adv Res, 2025, S2090-1232(25)00192-4
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Front Pharmacol, 2025, 16:1608156
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J Cell Mol Med, 2025, 29(11):e70641
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| S7724 |
Eprenetapopt (APR-246)
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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. It induces apoptosis and autophagy.
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Oncotarget, 2024, 15:614-633
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J Cell Mol Med, 2024, 28(9):e18374
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Cell Death Dis, 2023, 14(11):783
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| S8483 |
CBL0137 Hydrochloride
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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).
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Oncogene, 2025, 44(13):893-908
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Cancer Biol Ther, 2025, 26(1):2511301
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JCI Insight, 2023, 8(4)e154120
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| S8059 |
Nutlin-3a
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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.
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Nucleic Acids Res, 2025, 53(13)gkaf627
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Cell Rep Med, 2025, 6(8):102284
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Bone Res, 2025, 13(1):62
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| S7030 |
RG-7112
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RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.
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NPJ Aging, 2025, 11(1):6
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Int J Mol Sci, 2024, 25(7)3948
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bioRxiv, 2024, 2024.10.09.617493
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| S2930 |
Pifithrin-μ
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Pifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and this compound also inhibits HSP70 function and autophagy.
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Cell Death Dis, 2025, 16(1):42
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Front Nutr, 2025, 12:1663245
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Sci Adv, 2025, 11(12):eadq9111
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| S1172 |
Serdemetan (JNJ-26854165)
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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.
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Elife, 2025, 14e75393
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J Physiol, 2025, 603(19):5477-5508
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Signal Transduct Target Ther, 2022, 7(1):97
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| S2781 |
RITA
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RITA induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks, and this compound also inhibits MDM2-p53 interaction by targeting p53.
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Cell Death Discov, 2024, 10(1):381
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J Cancer, 2023, 14(2):200-218
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Theranostics, 2022, 12(9):4110-4126
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| S7723 |
PRIMA-1
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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.
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J Control Release, 2024, 371:111-125
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Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
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J Pers Med, 2022, 12(2)258
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| S8000 |
Tenovin-1
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Tenovin-1 protects against MDM2-mediated p53 degradation, which involves ubiquitination, and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2. This compound is also an inhibitor of dihydroorotate dehydrogenase (DHODH).
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J Pharm Biomed Anal, 2021, 201:114121
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J Transl Med, 2019, 17(1):76
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Int J Mol Med, 2019, 44(3):1091-1105
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