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XAV939

Inhibitor of TNKS, TNKS2, PARP1, PARP2

Structure

Information

  • TNKS
  • TNKS2
  • PARP1
  • PARP2
  • Inhibitor

In Vitro Validations

Uniprot ID: O95271
Target Class: Other post-translational modification
Target SubClass: PARP
Potency: Kd
Potency Value: 99 nM
Potency Assay: CY5-labeled XAV939 binding assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Poly [ADP-ribose] polymerase tankyrase-1, TNKS1, T ...

DOI Reference: 10.1038/nature08356

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency end-point : KD PARP1 1.2 uM
Potency assay (off target): No significant binding was detected against PARP2 using CY5-labeled XAV939 in binding assay.
Probe Selectivity in Vitro:
Potency assay, off target (cells): In HEK293 cells, XAV939 did not impact Cre, NF-kappaB or TGFbeta-dependent luciferase expression.
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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

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 inhibits PARP1 and PARP2 with similar potency to Tankyrase 1 and 2.

(last updated: 18 Jan 2017 )

SERP Ratings

In Cell Rating

SERP Comments:

Portal staff comment: A new publication appeared in December 2016 (PMID 28001384) indicating that XAV939 inhibits multiple PARP family proteins in addition to Tankyrase 1 & 2 (especially PARP1 and PARP2).

(last updated: 6 Feb 2017 )

SERP Ratings

In Cell Rating

SERP Comments:

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 targets.

(last updated: 15 Jun 2017 )