UNC8209 |
UNC8209 : Degrader (PROTAC) of TBK1
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| TBK1 |
|
Degrader (PROTAC)
up to 1 uM
Selectivity
In Cell Selectivity Assessment
Potency Assay Off-Target:
Western Blot of cell lysate
Selectivity Assessment Description:
UNC8209 displayed high selectivity for TBK1 degradation over its homolog IKKε, a common off-target o ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
To evaluate the selectivity of UNC8209, global proteomic profiling in UMRC2 cells treated with 1 μM ...
Selectivity Assessment Description:
Mass spectrometry analysis identified and quantified 8,307 proteins. Of these, 16 proteins were sign ...
Potency Cellular
In Vitro
TBK1
Mode of Action: Degrader (PROTAC)
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1016/j.chembiol.2026.03.013
In Vivo Validations
Mouse
Dose: 10 mg/Kg
Route of delivery:
Intraperitoneal
Cmax:
2300 ng/mL
Tmax:
2 h
DOI Reference: 10.1016/j.chembiol.2026.03.013
Negative Control Compounds
UNC8461
Notes: The negative control UNC8461 (NEG) compound failed to reduce TBK1 protein levels.
SMILES:
CN(C(C1CCC1)=O)CCCNC2=NC(NC3=CC=C(OCCOCCOCCOCCOCCOCCCOC4=C5C(C(N(C5=O)C6CCC(N(C)C6=O)=O)=O)=CC=C4)C=C3)=NC=C2Br
Chemical Information
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