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EP300-Deg-25a | EP300-Deg-25a : Degrader (PROTAC) of EP300, CREBBP
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
EP300
  • Inhibition:25.1%
  • Dmax:90.8 ± 1.1%
CREBBP
    • Dmax:59.6 ± 6.9%
    1 µM
    up to 1 uM, no hook effect up to 10 uM

    Selectivity

    Potency
    Cellular
    In Vitro

    EP300

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acsmedchemlett.6c00153

    CREBBP

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acsmedchemlett.6c00153

    Chemical Information

    Coming Soon...

    References

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    Expert Reviews

    by SERP
    (on 26 Aug 2026)
    Cellular Use Rating
    Compound 25a, a proline-based, cereblon-recruiting PROTAC, was identified as a degrader that preferentially promotes degradation of EP300 (p300) over its close paralog, CBP. EP300 is a lysine acetyltransferase...
    by SERP
    (on 31 Aug 2026)
    Cellular Use Rating
    The PROTAC EP300-Deg-25a degrades effectively degrades EP300 while largely sparing its close homolog CPB at low micromolar concentrations. Further selectivity data (e.g. global proteomics) and broader...
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