p53/mdm2

p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is a compound that inhibits the interaction between p53 and MDM2 proteins.

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

RO-5963 is a dual inhibitor of p53-MDM2 and p53-MDMX (IC50s: ~17 nM and ~24 nM, respectively).

Triglycidyl isocyanurate (Teroxirone) is a triazene triepoxide with antineoplastic and antiangiogenic 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. It induces cell apoptosis and can be used for cancer research[1][2]. Triglycidyl isocyanurate is also used in various polyester powder coatings in the metal finishing industry.

YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.

NSC 146109 hydrochloride is an activator of p53 targeting MDMX. NSC 146109 hydrochloride can be used for studies on breast cancer.

BH3I-1 (BHI1) is a Bcl-2 antagonist.

PhiKan 083, a carbazole derivative, exhibits potential as an eco-friendly dye with applications in the development of organic photovoltaic cells (OPVs).

NSC 66811is a novel inhibitor of the murine double minute 2 (MDM2)-p53 interaction. It binds to MDM2 with a Ki of 120 nM and activates p53 in cancer cells with a mechanism of action consistent with targeting the MDM2-p53 interaction.

Nutlin-3 is an MDM2 antagonist that inhibits MDM2-p53 interaction (Ki=90 nM) and activates p53. Nutlin-3 binds preferentially to the p53-binding pocket of MDM2, leading to stabilization of p53 and activation of the p53 pathway. Nutlin-3 has antitumor activity.

PK11000 is a p53 targeting compound, has anti-tumor activities through activation of unstable p53.

Siremadlin (NVP-HDM 201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.

Nutlin-3a is the active enantiomer of Nutlin-3, an MDM2 antagonist that inhibits MDM2-p53 interaction (Ki=90 nM) and activates p53. Nutlin-3a binds preferentially to the p53-binding pocket of MDM2, leading to stabilization of p53 and activation of the p53 pathway. Nutlin-3a has antitumor activity.

Navtemadlin (AMG232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction (IC50: 0.6 nM). It binds to MDM2 with a Kd of 0.045 nM.

p53-MDM2-IN-1 (Example 30), an inhibitor of the p53-MDM2/X protein interaction, exhibits a K i value of 23.35 µM and holds potential for applications in anti-tumor research.

p53-MDM2-IN-7 (compound 6d) (hydrochloride) is an inhibitor of the p53-MDM2 interaction, utilized in anticancer research.

p53-MDM2-IN-2 (Compound 5q) is an orally active p53-MDM2 inhibitor with a Ki value of 0.25 μM. It exhibits antitumor activity by inhibiting the NF-κB pathway.

p53-Mdm2 inhibitor 4 inhibits the p53-MDM2 protein-protein interaction.

p53-MDM2-IN-5 (compound 5a), a robust p53-MDM2 inhibitor, effectively induces apoptosis, autophagy, and DNA damage. It also causes cell cycle arrest at the S and G2/M phases and demonstrates anti-tumor activity.

MI-773 (SAR405838 (MI 773)) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

Vanillin (Zimco) is a single molecule extracted from vanilla beans and also a popular odor used widely in perfume, food and medicine.Vanillin can reversibly and non-competitively inhibit the cellulase activity at appropriate concentrations and the value of IC50 was estimated to be 30 g/L.Vanillin protects KSC from UVB irradiation and its effects may occur through the suppression of downstream step of MDM2 in UVB irradiation-induced p53 activation. Vanillin also inhibits yeast growth and fermentation.

USP7-IN-4(USP7 inhibitor ALM4) is a non-competitive, potent and selective inhibitor of USP7 (ubiquitin-specific protease 7) with an IC50 = 6 nM, up-regulates p53 and p21, down-regulates MDM2, increases the level of ubiquitination of MDM2, and exhibits anti-proliferative activity in a variety of cancer cell lines, with an EC50 = 2.0 nM in RS4;11 (acute lymphoblastic leukemia cell line) .

Brigimadlin (BI 907828) is an orally active and highly potent E3 ubiquitin-protein ligase MDM2-p53 antagonist with antitumor activity.Brigimadlin can be used to study metastatic BTC, PDAC, lung adenocarcinoma, or bladder cancer.

Nutlin-3b ((+)-Nutlin-3) is a p53/MDM2 antagonist or inhibitor (IC50: 13.6 μM), 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a.