JZ128 |
JZ128 : Covalent Inhibitor of PKN3
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary
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| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| PKN3 |
|
|
Covalent Inhibitor
up to 1 uM
Selectivity
In Cell Selectivity Assessment
Potency Assay Off-Target:
Proteome-wide selectivity of JZ128 was assessed in PC3 cells.
Selectivity Assessment Description:
Quantitative, dose-dependent competitive binding data for 686 reproducible JZ128-DTB-labeled cystein ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
In vitro kinase assays showed JZ128 to have a roughly 200 nM IC50 against SRC and RIPK2.
In Cell Selectivity Assessment
Potency Assay Off-Target:
KiNativ platform was used to interrogate JZ128 with respect to kinase inhibition.
Selectivity Assessment Description:
In total 292 kinases were detected in PC3 cells, with only three showing greater than 50% inhibition ...
Potency Cellular
In Vitro
PKN3
Mode of Action: Covalent Inhibitor
Structure-Activity-Relationship data available? No
DOI Reference: 10.1021/jacs.8b07911
Negative Control Compounds
JZ128-R
SMILES:
CN(CCCC(NC1=CC=C(C(NC2=CC=C(NC3=NC(C4=CNC5=C4C(C)=CC=C5)=NC=C3)C=C2)=O)C=C1)=O)C
Chemical Information
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