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XAV939 | Inhibitor of TNKS, TNKS2, PARP1, PARP2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
TNKS
  • Kd:99 nM
TNKS2
  • Kd:93 nM
PARP1
    PARP2
      Inhibitor
      --

      Selectivity

      In Vitro Selectivity Assessment

      Potency: KD - PARP1 1.2 uM

      Potency Assay Off-Target:
      No significant binding was detected against PARP2 using CY5-labeled XAV939 in binding assay.
      Selectivity Assessment Description:
      In Cell Selectivity Assessment
      Potency Assay Off-Target:
      In HEK293 cells, XAV939 did not impact Cre, NF-kappaB or TGFbeta-dependent luciferase expression.

      Potency
      Cellular
      In Vitro

      TNKS

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? No

      DOI Reference: 10.1038/nature08356

      TNKS2

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? No

      DOI Reference: 10.1038/nature08356

      PARP1

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? No

      DOI Reference: 10.1038/nature08356

      PARP2

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? No

      DOI Reference: 10.1038/nature08356

      Negative Control Compounds

      LDW643

      Orthogonal Probes def

      AZ6102
      JW55

      Chemical Information

      Molecular Formula C14H11F3N2OS
      SMILEs Oc1nc(-c2ccc(C(F)(F)F)cc2)nc2c1CSCC2
      InChI InChI=1S/C14H11F3N2OS/c15-14(16,17)9-3-1-8(2-4-9)12-18-11-5-6-21-7-10(11)13(20)19-12/h1-4H,5-7H2,(H,18,19,20)
      Molecular weight 312.05 Da
      AlogP 3.657300000000002
      HBond acceptors 3
      HBond donors 1
      Atoms 32

      References

      Publications

      Cross References

      GDSC1GDSC2

      Expert Reviews

      by SERP
      (on 18 Jan 2017 )
      Cellular Use Rating
      I strongly recommend performing a dose-response for the cell line in question and instituting an assay for inhibition of PARP1 and/or PARP2 once the concentration of XAV939 has been selected. XAV939...
      by SERP
      (on 6 Feb 2017 )
      Cellular Use Rating
      ...
      by SERP
      (on 15 Jun 2017 )
      Cellular Use Rating
      As the recent publication (https://www.ncbi.nlm.nih.gov/pubmed/?term=28001384) shows, this compound is a promiscuous Tankyrase inhibitor and, hence, is not a good tool to probe the role of individual...
      Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria