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MI-888 | MI-888 : Antagonist of MDM2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
MDM2
  • Ki:0.44 nM
  • IC50:0.08 uM
Antagonist
1-100 nM

Selectivity

Potency
Cellular
In Vitro

MDM2

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

In Vivo Validations

Sprague Dawley rat, SCID mice
Dose: 25 mg/kg (rat)
Route of delivery: Oral
Plasma half life: 3.2 h (rat)
Organ of interest (O): SJSA-1 xenograft (SCID mice, 10-100 mg/kg)
Target engagement assay: In xenograft, MI-888 increased expression of p53, MDM2 and p21 proteins.

Reference: --

Orthogonal Probes def

RO5353
AMG232
AM-6761

Chemical Information

Molecular Formula C28H32Cl2FN3O3
SMILEs CC(C)(C)C[C@@H]1N[C@@H](C(=O)N[C@H]2C[C@@](C)(O)C2)[C@H](c2cccc(Cl)c2F)[C@]12C(=O)Nc1cc(Cl)ccc12
InChI InChI=1S/C28H32Cl2FN3O3/c1-26(2,3)13-20-28(17-9-8-14(29)10-19(17)33-25(28)36)21(16-6-5-7-18(30)22(16)31)23(34-20)24(35)32-15-11-27(4,37)12-15/h5-10,15,20-21,23,34,37H,11-13H2,1-4H3,(H,32,35)(H,33,36)/t15-,20-,21-,23+,27+,28+/m0/s1
Molecular weight 547.18 Da
AlogP 4.9124
HBond acceptors 6
HBond donors 4
Atoms 69

References

Publications

Cross References

canSARChEMBLBindingDBBindingDB

Vendors

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Expert Reviews

by SERP
(on 26 Jul 2017)
Cellular Use Rating
In Model Organisms
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...
by SERP
(on 28 Jul 2017)
Cellular Use Rating
In Model Organisms
MI-888 is potent against MDM2, but its broader receptor profile is not reported.
by SERP
(on 31 Jul 2017)
Cellular Use Rating
In Model Organisms
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.
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria