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p300-Deg-27 | p300-Deg-27 : Degrader (PROTAC) of EP300
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
EP300
  • IC50:12.6 nM
  • IC50:14.8 nM
  • DC50:22.5 nM
up to 100 nM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
Proteome-wide analysis of protein levels in MM1.S cells treated with 3 nM of cpd 27 for 6 h.
Selectivity Assessment Description:
Results revealed a profound degradation of the p300 protein with no major impact on CBP protein leve ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
To investigate whether distinct ubiquitination sites influence degradation selectivity, proteome-wid ...
Selectivity Assessment Description:
Regioselective ubiquitination of p300 K1167 contribute to paralog selectivity.
In Cell Selectivity Assessment
Potency Assay Off-Target:
High-throughput PRISM screen using 906 cancer cell lines treated with Degrader 27 for 5 days.
Selectivity Assessment Description:
After correlating the AUC of the dose-response curve with top gene dependencies identified through g ...

Potency
Cellular
In Vitro

EP300

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41467-026-72635-x

In Vivo Validations

Mouse
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 6.8 h
Systemic clearance: 0.38 L/hr/kg
Area Under the Curve:: 2660 ng*hr/mL
Volume of Distribution at Steady-State: 2.4 L/Kg

DOI Reference: 10.1038/s41467-026-72635-x

Dose: 1 mg/Kg
Route of delivery: Intraperitoneal
Plasma half life: 5.8 h
Cmax: 306 ng/mL
Tmax: 3.0 h
Area Under the Curve:: 2900 ng*hr/mL
Bioavailability: >100%

DOI Reference: 10.1038/s41467-026-72635-x

Chemical Information

Molecular Formula C50H58F2N10O5
SMILEs CNC(=O)N1CCc2c(c(N3CCCc4cc(-c5cnn(CC(=O)N[C@H]6CC[C@H](CCc7cc(N8CCC(=O)NC8=O)c8ccccc8c7)CC6)c5)c(C(F)F)cc43)nn2C2CCOCC2)C1
InChI InChI=1S/C50H58F2N10O5/c1-53-49(65)58-19-14-42-41(29-58)48(57-62(42)37-16-21-67-22-17-37)60-18-4-6-34-25-39(40(47(51)52)26-43(34)60)35-27-54-59(28-35)30-46(64)55-36-12-10-31(11-13-36)8-9-32-23-33-5-2-3-7-38(33)44(24-32)61-20-15-45(63)56-50(61)66/h2-3,5,7,23-28,31,36-37,47H,4,6,8-22,29-30H2,1H3,(H,53,65)(H,55,64)(H,56,63,66)/t31-,36-
Molecular weight 916.46 Da
AlogP 7.724800000000008
HBond acceptors 15
HBond donors 3
Atoms 125
PAINS * Yes

* This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )

References

Publications

Cross References

canSAR: 7719223 canSAR: 29

Expert Reviews

by SERP
(on 17 Aug 2026)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
by SERP
(on 18 Aug 2026)
Cellular Use Rating
In Model Organisms
Highly selective and potent EP300 degrader which utilizes CRBN ligase as the E3 ligase. Numerous orthogonal methods in vitro show that it degrades EP300 with low nM potency without degrading its closely...
by SERP
(on 31 Aug 2026)
Cellular Use Rating
In Model Organisms
p300-Deg-27 is a CRBN based PROTAC that degrades p300 with a DMax of 86% and has selectivity over the paralog CBP. Recommended for use up to 100nM as the compound demonstrates a hook effect at higher concentrations....
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