Inhibitor of TNKS, TNKS2
In Vitro Validations
Uniprot ID: O95271
Target Class: Other post-translational modification
Target SubClass: PARP
Potency: IC 50
Potency Value: 1900 nM
Potency Assay: Biochemical PARylation assays
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: Yes
Poly [ADP-ribose] polymerase tankyrase-1, TNKS1, T ...
DOI Reference: 10.1158/0008-5472.CAN-11-3336
In Cell Validations
In Vivo Data
No in Vivo Validations
Off-Target Selectivity Assesments
Potency end-point : IC50 PARP1 >20 uM
Potency assay (off target): Biochemical PARylation assay.
Probe Selectivity in Vitro:
JW55 had no activity against 8 ARTD isoenzymes.
Probe Selectivity in Cell:
In Shh-Light II cells (Gli1-Luc reporter) and in TNFalpha-activated HEK293 cells (NF-kappaB luciferase reporter), JW55 had no effect on reporter expression up to 10 uM. In HEK293 cells, JW55 dose-dependently countered LiCl-induced Wnt signaling, and this activity was overcome by expression of dominant active beta-catenin. In SW480 and HCT-15 cells, JW55 dose-dependently decreased SuperTop-luciferase reporter gene expression and stabilized AXIN2.
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