mdm2

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.

Triptolide (PG490) belongs to the tricyclic diterpenoid group of natural products and is an inhibitor of NF-κB activation. Triptolide exhibits immunosuppressive, anti-rheumatic, anti-inflammatory, anti-proliferative and anti-tumor activities.

PROTAC MDM2 Degrader-4, designed using PROTAC technology, combines a potent MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase to degrade MDM2[1].

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.

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

MDM2-IN-26 (compound A3) is an inhibitor of MDM2 that facilitates the activation of p53's tumor suppressor functions by inhibiting the MDM2-p53 interaction, with MDM2 being the primary negative regulator of p53. This compound is utilized in cancer research [1].

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

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

MDM2-p53-IN-1b is the MDM2-p53 interaction inhibitor.

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.

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

PROTAC MDM2 Degrader-2, designed using PROTAC technology, functions as a MDM2 degrader. It consists of a highly potent MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase, facilitating the degradation of MDM2[1].

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

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].

PROTAC MDM2 Degrader-1 is a chemical compound that employs PROTAC technology to degrade MDM2, comprising a highly effective MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase[1].

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

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 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].

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