MI-888
MI-888 : Antagonist of MDM2
Structure
In Cells
In Model Organisms
SERP ratings and comments
SERP Ratings
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
SERP Comments:
MI-888 is potent against MDM2, but its broader receptor profile is not reported.
(last updated: 28 Jul 2017 )
SERP Ratings
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 )