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JW55 | Inhibitor of TNKS, TNKS2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (1 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
TNKS
  • IC 50:1900 nM
  • IC 50:470 nM
TNKS2
  • IC 50:830 nM
  • IC 50:470 nM
Inhibitor
--

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - PARP1 >20 uM

Potency Assay Off-Target:
Biochemical PARylation assay.
Selectivity Assessment Description:
JW55 had no activity against 8 ARTD isoenzymes.
In Cell Selectivity Assessment
Selectivity Assessment Description:
In Shh-Light II cells (Gli1-Luc reporter) and in TNFalpha-activated HEK293 cells (NF-kappaB lucifera ...

Potency
Cellular
In Vitro

TNKS

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1158/0008-5472.CAN-11-3336

TNKS2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1158/0008-5472.CAN-11-3336

Orthogonal Probes def

XAV939
AZ6102

Chemical Information

Molecular Formula C25H26N2O5
SMILEs COc1ccc(C2(CNC(=O)c3ccc(NC(=O)c4ccco4)cc3)CCOCC2)cc1
InChI InChI=1S/C25H26N2O5/c1-30-21-10-6-19(7-11-21)25(12-15-31-16-13-25)17-26-23(28)18-4-8-20(9-5-18)27-24(29)22-3-2-14-32-22/h2-11,14H,12-13,15-17H2,1H3,(H,26,28)(H,27,29)
Molecular weight 434.18 Da
AlogP 0.0
HBond acceptors 7
HBond donors 2
Atoms 58

References

Publications

Cross References

canSARChEMBLBindingDBPDB

Vendors

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Expert Reviews

by SERP
(on 12 Aug 2016 )
Cellular Use Rating
In Model Organisms
More potent analogs of JW55 are already available (doi:10.1016/j.bmcl.2015.12.018). Citation of this paper regarding moderate potency: "In vitro inhibition, as measured by biochemical assay complemented...
by SERP
(on 17 Aug 2016 )
Cellular Use Rating
Weak probe with iffy biochemical support. Stay away!
by SERP
(on 9 May 2019 )
Cellular Use Rating
Even though authors have demonstrated that JW55 is a potent inhibitor of the Wnt canonical signalling by facilitating beta-catenin degradation, not enough data was presented on the efficacy of JW55...
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