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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

    Note: This is not an exhaustive list and does not indicate endorsement by the portal.

    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