p53

HLI373 dihydrochloride is an efficacious Hdm2 inhibitor.

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.

MS7972 is a small molecule that blocks human p53 and CREB binding protein association. MS7972 can almost completely block this BRD interaction at 50 μM.

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

MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.

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.

MB710, an aminobenzothiazole derivative, is a stabilizer of oncogenic p53 mutation Y220C. MB710 binds tightly to the Y220C pocket and stabilizes p53-Y220C, with a Kd of 4.1?μM. MB710 shows anticancer activity in p53-Y220C cell lines.

MD-222 is the first-in-class highly potent PROTAC degrader of MDM2. MD-222 consists of ligands for Cereblon and MDM2. MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53 in cells. MD-222 has anticancer effects.

6α-Hydroxy Paclitaxel-d5 is the deuterium labeled 6α-Hydroxy paclitaxel. 6α-Hydroxy paclitaxel is a primary metabolite of Paclitaxel. 6α-Hydroxy paclitaxel retains a time-dependent effect on organic anion-transporting polypeptides 1B1/SLCO1B1 (OATP1B1) with similar inhibition potency to Paclitaxel, whereas it no longer showed time-dependent inhibition of OATP1B3. 6α-Hydroxy paclitaxel can be used for the research of cancer.

Cjoc42 is a compound capable of binding to gankyrin. Cjoc42 inhibits gankyrin activity in a dose-dependent manner. Cjoc42 prevents the decrease in p53 protein levels normally associated with high amounts of gankyrin. Cjoc42 restores p53-dependent transcription and sensitivity to DNA damage.

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

SLMP53-1 is a wild-type and mutant p53 reactivator with promising antitumor activity. SLMP53-1 mediates the reprograming of glucose metabolism in cancer cells. SLMP53-1 depletes angiogenesis, decreasing endothelial cell tube formation and vascular endothelial growth factor (VEGF) expression levels.

ADH-6 TFA is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 TFA 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 TFA has the potential for the research of cancer diseases.

P53R3 is a potent p53 reactivator and restores sequence-specific DNA binding of p53 hot spot mutants, including p53R175H, p53R248W and p53R273H. P53R3 induces p53-dependent antiproliferative effects with much higher specificity than PRIMA-1. P53R3 enhances the recruitment of wild-type p53 and p53M237I to several target gene promoters. P53R3 strongly enhances the mRNA, total protein and cell surface expression of the death receptor death receptor 5 (DR5). P53R3 is used for cancer research.

MDM2-p53-IN-16 is a MDM2-p53 complex inhibitor with an IC50 value of 4.3 nM for dissociating the human MDM2-p532 complex. It can reactivate p53 and induce apoptosis and cell cycle arrest in glioblastoma multiforme (GBM) cells. MDM2-p53-IN-16 can be used for cancer research purposes.

p53 Activator 7 is a p53 mutant Y220C (MDM-2/p53) activator with an EC50 of 104 nM. It can bind to p53 mutants and restore their ability to bind DNA (WO2022213975A1; Example B-1).

Sulanemadlin is a membrane-permeable, potent macrocyclic peptidomimetic compound based on the p53 target, and is a stable α-helical peptide.

MMRi64 disrupts Mdm2-MdmX interactions.

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

U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells.

p53 Activator 3 (compound 87A) is a potent p53 activator with a SC150 value of <0.05 mM.

MS78 is an acetylation targeting chimera (AceTAC) that acetylates the p53 tumor suppressor protein.