RG7388

Antagonist of MDM2

Structure

Information

Protein target names: MDM2

Mechanism of action: Antagonist

Recommended in-cell concentration:
10-500 nM

In Vitro Validations

Uniprot ID: Q00987
Target Class: Other post-translational modification
Target SubClass: E3 ubiquitin ligase
Potency: IC50
Potency Value: 6 nM
Potency Assay: Homogenous time-resolved fluorescence binding assay.
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: Yes, see J Med Chem paper
Target aliases:
E3 ubiquitin-protein ligase Mdm2, MDM2, MDM2_HUMAN ...

DOI Reference: 10.1021/jm400487c

Uniprot ID: Q00987
Target Class: Other post-translational modification
Target SubClass: E3 ubiquitin ligase
Potency: Kd
Potency Value: 9.79 nM
Potency Assay: Biacore binding assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
E3 ubiquitin-protein ligase Mdm2, MDM2, MDM2_HUMAN ...

DOI Reference: 10.1021/jm400487c

In Cell Validations

In Vivo Data

I have extra information to add

SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 17 Aug 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

RG7388 is a second-generation inhibitor of the protein-protein interaction that occurs between wild type p53 (a potent tumor suppressor) and the E3 ubiquitin ligase MDM2. High levels of MDM2 are found in several tumor types, resulting in the destruction of p53. Inhibition of this interaction with chemical probes such as RG7388 can restore wild-type p53 activity in cells. Medicinal chemistry efforts to improve the original 'Nutlin' class of MDM2 inhibitors have yield compounds such as RG7388, with improved activity and pharmacokinetic properties.

(last updated: 17 Aug 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

Potent and optimised MDM2-p53 antagonist that entered into clinical trials. In general, there is only very limited data available with regard to the selectivity of this compound. However, in contrast to some other published compounds from this class, RG7738 appears to only exhibit off-target effects on MDR-1 at concentrations of 5 µM.

(last updated: 16 Nov 2020 )