A highly potent, selective mutant p53 (R175H, R249S, R273H, R273C) reactivator.

A novel small molecule that overcomes HdmX-mediated p53 repression, binds directly to HdmX (Kd=450 nM) to prevent p53-HdmX complex formation.

CB-002 is a novel small molecule that restores p53 function in mutant p53-expressing colorectal cancer cells without toxicity to normal human fibroblasts; increases expression of endogenous p53 target genes NOXA, DR5, and p21 and cell death; decreases the stability of mutant p53 in RXF393 cancer cells and an exogenously expressed R175H p53 mutant in HCT116 p53-null cells.

A potent and orally active p53-MDM2 interaction inhibitor with IC50 of 2.4 nM.

A potent MDM2-p53 interaction inhibitor with remarkable biochemical (HTRF IC50=0.1 nM), cellular potency (SJSA-1 EdU IC50=16 nM), and favorable pharmacokinetic properties.

A potent MDM2-p53 interaction inhibitor with remarkable biochemical (HTRF IC50=0.4 nM), cellular potency (SJSA-1 EdU IC50=25 nM), and favorable pharmacokinetic properties.

A potent small molecule inhibitor that binds and disrupts the MDM2/MDMX-p53 interaction with IC50 of 0.19 uM and 19.7 uM, respectively..

RO-5963 is an inhibitor of the interaction of both MDM2 and MDMX with p53.

A potent, highly selective, orally active MDM2-p53 interaction inhibitor with IC50 of 4 nM.

A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 6 nM.

A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 7 nM.

A potent, selective, orally bioavailable MDM2-p53 interaction inhibitor with HTRF IC50 of 1.1 nM, SJSA-1 EdU IC50 of 68 nM.

A small molecule inhibitor of HDM2-p53 interaction with FP IC50 of 0.7 uM.

A small molecule inhibitor of MDM2-p53 protein-protein interaction with IC50 of 16 uM..

A small molecule inhibitor of MDM2-p53 protein-protein interaction with IC50 of 5.3 uM in ELISA assay.

AMG232 is a potent, selective and orally bioavailable inhibitor of MDM2−p53 interaction with IC50 value of 9.1 nM in EdU cells .

COTI-2 is a small molecule candidate anti-cancer drug which can convert mutant p53 to wild-type conformation.

Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis.

HDM201 is an orally bioavailable human double minute 2 homolog (HDM2) inhibitor with potential antineoplastic activity.

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.

MB710 is a small-molecule p53 mutant Y220C stabilizer, binds tightly to the Y220C pocket and stabilizes p53-Y220C in vitro..

MB725 is a small-molecule p53 mutant Y220C stabilizer, induces selective viability reduction in several p53-Y220C cancer cell lines (Huh7 cell IC50=10 uM).

MI-77301 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

MX69 is the MDM2/XIAP inhibitor, used for cancer treatment.

NSC 66811 is a potent MDM2 inhibitor (Ki = 120 nM).

NSC319726 is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.

NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway.The EC50 of NSC59984 in most cancer cells is significantly lower than those of normal cells, with EC50 of 8.38 μM for p53-null HCT116 cells.

Nutlin 3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.

Nutlin-3a is arbitrarily referred to as enantiomer a because it appears as the first peak from chiral purification of racemic nutlin-3 and its absolute stereocenter assignment is not known.

Nutlin-3b is 150-fold less potent as an inhibitor of p53-MDM2 interaction than (−)-nutlin-3, demonstrating an IC50 value of 13.6 µM.

Pifithrin-β HBr (Cyclic Pifithrin-α HBr) is a potent p53 inhibitor with IC50 of 23 uM in an antiproliferative assay in the human ovarian carcinoma cell line, IGROV-1.

PRIMA-1 is a mutant p53 reactivator, restores the sensitivity of TP53 mutant-type thyroid cancer cells to the histone methylation inhibitor 3-Deazaneplanocin A.

PRIMA-1MET is methylated derivative of PRIMA-1. It can restore mutant p53 activity.

RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor.

RO8994 is a potent and selective spiroindolinone MDM2 inhibitor for cancer therapy.

SJ-172550 is the first MDMX inhibitor with EC50 of 0.84 uM; binds reversibly to MDMX and effectively kills retinoblastoma cells in which the expression of MDMX is amplified.

SP 141 is a cell-permeable inhibitor of Mdm2 (Ki = 28 nM).

Tenovin-3 is a small molecule activator of p53 transcriptional activity.

YH239-EE, ethyl ester of the free carboxylic acid compound YH239, is a potent p53-MDM2 antagonizing and apoptosis-inducing agent

PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 by covalent cysteine modification, without compromising DNA binding.

Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED50=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue.

MDM2-IN-1 (Compound 30) is a synthetic MDM2-p53 interaction (MDM2) inhibitor and contains the trans (D-)configuration.

Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis.

Triglycidyl isocyanurate (TGIC; Teroxirone) is a triazene triepoxide with antiangiogenic and antineoplastic activities. Triglycidyl isocyanurate inhibits the growth of non-small-cell-lung cancer cells via?p53 activation. Triglycidyl isocyanurate induces cell apoptosis. Triglycidyl isocyanurate can be used for cancer research.

Amifostine thiol (WR-1065) is an active metabolite of the cytoprotector Amifostine. Amifostine thiol is a cytoprotective agent with radioprotective abilities. Amifostine thiol activates p53 through a JNK-dependent signaling pathway.

p53 and MDM2 proteins-interaction-inhibitor (chiral) (Compound 32) is an of the interaction between p53 and MDM2 proteins.

p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is an of the interaction between p53 and MDM2 proteins.

MDM2-IN-21 is a potent MDM2 inhibitor. MDM2-IN-21 can be used for the research of cancer.

Teprasiran (QPI-1002) is a small interfering RNA that temporarily inhibits p53-mediated cell death that underlies acute kidney injury (AKI).

Sanggenol L induces caspase-dependent and caspase-independent apoptosis in melanoma skin cancer cells. Sanggenol L induces of apoptosis via suppression of PI3K/Akt/mTOR signaling and cell cycle arrest via activation of p53 in p

MA242 free base is a specific dual inhibitor of MDM2 and NFAT1. MA242 free base directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 free base induces apoptosis in pancreatic cancer cell lines regardless of p53 status.

ADH-6 is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 has the potential for the research of cancer diseases.

PK9327 is a small-molecule stabilizer targeting cavity-creating p53 cancer mutations.

Mutant p53 modulator-1 is a mutant p53 modulator. Mutant p53 modulator-1 reduces the progression of cancers that contain a p53 mutation (extracted from patent WO2021231474A1, compound 231B).

NSC405640 is a potent inhibitor of the MDM2-p53 interaction. NSC405640 rescues structural p53 mutations. NSC405640 selectively inhibits the growth of cell lines with wild-type p53.

NSC194598 is a specific small molecule inhibitor that inhibits p53 sequence-specific DNA binding in vitro (IC50=180 nM) and in vivo.

A novel small-molecule dual inhibitor of p53-MDM2/X interactions by potentially binding to p53, without effect on other MDM; causes growth inhibition, mediated by p53 stabilization and upregulation of p53 transcriptional targets involved in cell cycle arrest and apoptosis; shows a p53-dependent antitumor activity in human tumor xenograft mice models; a novel p53 activator.

ALRN-6924 (ALRN6924) is a potent dual inhibitor of MDM2/MDMX.ALRN-6924 demonstrated potent anti-proliferative activity in a dose-dependent manner in two ER+ cell lines with WT TP53, MCF-7 and ZR-75-1, with IC50 values of 113 nM and 500 nM respectively.The combination of ALRN-6924 and chemotherapeutic agents synergistically inhibit cell proliferation in vitro, ALRN-6924 combined with paclitaxel reactivates p53 and induces cell cycle arrest and apoptosis in vitro.ALRN-6924 mutually enhances both paclitaxel and eribulin antitumor efficacy and inhibits tumor growth in vivo.

H203 is a potent dual Mdm2/MdmX inhibitor with Ki of 2/11 nM, respectively; H203 significantly reduced cell viability in the cells overexpressing both Mdm2 and MdmX, and a significant and dose-dependent decrease in cell number in H203-treated cells lacking Mdm2 or MdmX. H203-mediated decrease in cell viability is strictly p53-dependent and H203 affects MdmX more specifically than nutlin-3a. H203 induced the expression of the p21 gene but not the p53 gene in treated cancer cells.

H210 is a potent dual Mdm2/MdmX inhibitor with Ki of 9.66/2.89 nM, respectively.

NSC90616 is a mutant p53 rescue compound.

BI-0282 (Compound 1) is a potent MDM2-p53 interaction inhibitor.

C16-Ceramide is a natural small molecule activating p53 through the direct and selective binding.

GN25 is a specific p53-Snail binding inhibitor with antitumor effects.

3-Morpholinosydnonimine (SIN-1; Linsidomine) is a spontaneous ROS/RNS generator and a peroxynitrite donor. 3-Morpholinosydnonimine inhibits hypertrophic chondrocytes activity and induces necrosis. 3-Morpholinosydnonimine induces p53-dependent apoptosis, induces p53 accumulation and activates MAPK phosphorylation.

BAY 1892005 is a small molecule that modulate mutant p53 condensation and nuclear accumulation, binds covalently to mutant p53R175H and p53Y220C and shows stabilization of p53WT and p53Y220C, exhibits anti-proliferative activity in a set of cell lines wit

BAY 249716 is a small molecule that modulate mutant p53 condensation, showed significant stabilization of all three p53 protein variants, p53WT p53R175H and p53Y220C.

GY1-22 is a small molecule inhibitor against DNAJA1-mutP53R175H interacting pocket, reduces mutp53 protein expression in colon cancer cell line with p53R175H mutation.

RPL11-MDM2 inhibitor S9 (J012-3168) is a small-molecule RPL11 mimetic and potential inhibitor of RPL11-MDM2 interaction, directly binds MDM2 and induces p53 stabilization and activation.

K-181 is a specific small-molecule Protein-Protein Interaction (PPI) inhibitor of Mdmx-p53 interaction, exhibits neuroprotective effects on ischemic stroke by disrupting Mdmx-p53 interaction and inhibiting HDAC6 activity.

MMRi67 is a potent E3 ligase inhibitor of the MDM2-MDM4 E3 complex, inhibits RING-RING interaction of MDM4 and MDM2B with Kd of 896 nM.

MMRi71 is a small molecule inhibitor of the E3 ligase activity of MDM2-MDM4, and an inducer of MDM4 and FTH1 dual protein degradation and p53-independent apoptosis in leukemia cells.

Morncide (Morn3 (222-237)) is a cell-penetrating, 16-AA Morn3-targeting peptide that disrupts the interaction between p53 and Morn3-mediated complex, Morncide peptide stabilizes and reactivates p53 in cancer cells.

NSC146109 (XI-011) is a small-molecule p53 activator, induces apoptosis of breast cancer cells through inhibiting MDMX (MDM4) expression.

ReACp53 is a cell-penetrating 17-residue peptide designed to inhibit p53 amyloid formation, rescues p53 function in cancer cell lines.

UC2288 is a small molecule p21 inhibitor, attenuates p21 protein abundance at 10 µM, independently of p53 activity and at the level of transcription or post-transcription.

UCI-LC0019 is a specific small molecule that restores mutant p53 activity by targeting the cryptic L1/S3 pocket of p53, directly binds to mutant p53 and restores wild-type-like conformation of mutant p53R175H.

UCI-LC0023 is a small molecule that restores mutant p53 activity by targeting the cryptic L1/S3 pocket of p53, directly binds to mutant p53 and restores wild-type-like conformation of mutant p53R175H.