MI-888

MI-888 : Antagonist of MDM2

Structure

Information

  • MDM2
  • Antagonist

In Vitro Validations

Uniprot ID: Q00987
Target Class: Other post-translational modification
Target SubClass: E3 ubiquitin ligase
Potency: Ki
Potency Value: 0.44 nM
Potency Assay: Fluorescence polarization assay with MDM2 protein and p53 peptide.
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 ...

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

The probe has been demonstrated to be a highly potent inhibitor of the MDM-p53 interaction by several in vitro and in vivo approaches. A couple of caveats are appropriate to note, which do not necessarily diminish the validity of the probe but should be borne in mind by users: 1) Selectivity in a cellular setting setting is demonstrated to be >100-fold for the HCT-116 cell line with wild-type p53 versus the isogenic p53-deleted cell line, but a wider selectivity profile at other molecular targets has not been reported. 2) The probe demonstrates excellent in vivo rat PK parameters and demonstrates excellent in vivo activity in a mouse xenograft model, but the mouse PK profile was not reported.

(last updated: 26 Jul 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

MI-888 is potent against MDM2, but its broader receptor profile is not reported.

(last updated: 28 Jul 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

Based on the data published in JMC, 2013, 56, 5553, this is a very nice tool molecule with potency and DMPK properties that are appropriate for multi-day dosing. Nice design.

(last updated: 31 Jul 2017 )