mdm 2

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

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

MDM2-IN-21 is a potent MDM2 inhibitor [MOI-115] applicable for cancer research.

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.

p53-MDM2-IN-6, an LSM-83177 hydrazone analog, acts as an efficacious p53-MDM2 inhibitor with an IC50 of 11.08 µg/mL. This compound inhibits the p53-MDM2 interaction leading to an increase in p-53 levels while concurrently decreasing GST enzyme expression. It halts the cell cycle at the S phase and induces early and late apoptosis (Apoptosis), exhibiting antiproliferative activity against the HT29 cell line with an IC50 of 10.44 µg/mL. p53-MDM2-IN-6 holds promise for research in colorectal cancer.

MDM2ligand 4 is a ligand of MDM2 and can be used in the synthesis of the PROTAC degrader [KT-253].

MDM2-IN-23 is an inhibitor of MDM2, exhibiting an IC50 of 60.09 μM against MCF-7 cells.

MDM2-IN-24 (Compound A3f) exhibits characteristics of MDM2 inhibition and MDMX activation in triple-negative breast cancer cells, showing pro-apoptotic (apoptosis) and anti-proliferative activities.

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.

CDK2/MDM2-IN-1 (III-13) is a dual inhibitor targeting both CDK2 and MDM2, exhibiting an IC50 value of 2.60 nM against CDK2, and demonstrating antitumor activity.

MDM2-IN-27 primarily targets the MDM2 protein with a Ki value of 0.4 nM. By blocking the negative regulation of p53 by MDM2, it activates the tumor-suppressing activity of p53 and induces apoptosis.

rel-MDM2/4-p53-IN-3 is an MDM2/4-p53 protein-protein interaction (PPI) inhibitor that acts on MDM2-p53 and MDM4-p53 with IC50 values of 18.5 nM and 14.8 nM, respectively. rel-MDM2/4-p53-IN-3 can be used to study cancers, such as colon cancer.

rel-MDM2/4-p53-IN-2 (2q) is a potent dual MDM2/MDM4 inhibitor and p53 activator that acts on both the MDM2-p53 complex (IC50: 70.7 nM) and the MDM4-p53 complex (IC50: 81.4 nM). rel-MDM2/4-p53-IN-2 is capable of regulating cell cycle, induce apoptosis, and exhibit anti-cancer effects.

MDM2-p53-IN-16 is a potent inhibitor of the MDM2-p53 complex, with an IC 50 value of 4.3 nM for the dissociation of the human p53/MDM2 complex. It effectively reactivates p53, leading to apoptosis and cell-cycle arrest in Glioblastoma Multiforme (GBM) cells, positioning it as a valuable agent for cancer research.

MDM2/4-p53-IN-2 (2q) is a potent dual inhibitor of MDM2/MDM4 and activator of p53, demonstrating IC50 values of 70.7 nM for MDM2-p53 and 81.4 nM for MDM4-p53 complexes. It facilitates cell cycle regulation, promotes apoptosis, and exhibits anticancer properties [1].

MDM2/4-p53-IN-3, an inhibitor of MDM2/4-p53 protein-protein interactions (PPIs), exhibits potent activity with IC50 values of 18.5 nM for MDM2-p53 and 14.8 nM for MDM4-p53. This compound is applicable in cancer research, including studies on colon cancer [1].

MDMX/MDM2-IN-2 is a potent dual inhibitor of p53-MDM2/MDMX, with dissociation constants (Kis) of 0.23 μM for MDM2 and 2.45 μM for MDMX. It disrupts the interaction between p53 and MDM2 proteins, reinstating p53 functionality to induce cell cycle arrest and apoptosis. Additionally, this compound impedes cell migration and invasion, exhibiting notable antitumor activity [1].

MDM2/XIAP-IN-2 is a dual inhibitor targeting murine double minute 2 (MDM2) and X-linked inhibitor of apoptosis protein (XIAP), promoting MDM2 degradation and impeding XIAP mRNA translation, thereby inhibiting cancer cell proliferation. It exhibits potent activity against the acute lymphoblastic leukemia cell line EU-1, with an IC50 of 0.3 μM [1].

MDM2/XIAP-IN-3 (compound 3e), a dual inhibitor of MDM2 and XIAP, reduces MDM2 and XIAP protein levels while increasing p53 expression, ultimately inhibiting cancer cell proliferation and inducing apoptosis [1].

MDM2/XIAP-IN-1 (compound 14) is an orally active dual inhibitor of MDM2 and XIAP, displaying anti-cancer activity with an IC50 of 0.3 μM and potential applications in cancer research [1].

MDM2-p53-IN-18, also known as Compd A-7b, is an inhibitor of the MDM2-p53 interaction [1].

MDM2-p53-IN-20 (Compd B-11j) is a synthetic inhibitor of the MDM2-p53 interaction, which is crucial in cancer [1].