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KT-253 | KT-253 : Degrader (PROTAC) of MDM2
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
MDM2
    • DC50:0.4 nM
    • IC50:0.3 nM
    Degrader (PROTAC)
    up to 100 nM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    The selectivity of KT-253 for MDM2 was investigated using tandem mass tag–based deep proteome profil ...

    Potency
    Cellular
    In Vitro

    MDM2

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1158/1535-7163.MCT-24-0306

    Negative Control Compounds

    Compound 1
    Notes: Compound 1 is the KT-253 analog that lacks the ability to bind CRBN.
    SMILES: CN1C2=C(N(C3CCC(N(C)C3=O)=O)C1=O)C=CC(C4CCN(C(C5CCC(NC([C@H]6[C@H](C7=C(F)C(Cl)=CC=C7)[C@]8(C9(CCCCC9)N6)C%10=C(NC8=O)C=C(Cl)C=C%10)=O)CC5)=O)CC4)=C2

    Chemical Information

    Coming Soon...

    References

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    Expert Reviews

    by SERP
    (on 24 Feb 2026 )
    Cellular Use Rating
    ( The reviewer did not leave any comments )
    by SERP
    (on 6 Apr 2026 )
    Cellular Use Rating
    KT-253 is a heteorbifunctional degrader of MDM2 through the recruitment of cereblon (CRBN) with a DC50 of 40 nM and a DC90 ~500-1000nM. KT-253 has advanced to phase 1 clinical studies. KT-253 has good...
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