p300-Deg-27 |
p300-Deg-27 : Degrader (PROTAC) of EP300
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| EP300 |
|
|
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
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