General
Preferred name
XAV939
Synonyms
XAV 939 ()
NVP-XAV939 ()
284028-89-3 ()
XAV-939 ()
P&D ID
PD011102
CAS
284028-89-3
Tags
available
probe
Probe info
Probe type
calculated probe
experimental probe
Probe sources
Chemical Probes.org
Tool Compound Set
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
14
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
COMMENT
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. Jan 19 2017 - 1:59pm; 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). Jan 19 2017 - 3:52pm; 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. Feb 7 2017 - 12:18pm
MOA
Inhibitor
(Chemical Probes.org)
DESCRIPTION
Potent tankyrase inhibitor
(Tocriscreen Plus)
DESCRIPTION
Endothelial lipase and lipoprotein lipase inhibitor
(Tocris Bioactive Compound Library)
DESCRIPTION
Tankyrase inhibitor; inhibits wnt signaling
(Tocriscreen Total)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
2
Organisms
0
Compound Sets
18
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
Chemical Probes.org
Drug Repurposing Hub
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
NURSA ligand set
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
Tocriscreen Total
Tool Compound Set
Welcome Trust Cancer Drugs
ZINC Tool Compounds
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
25
Molecular Weight
312.05
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
1
Rotatable Bonds
1
Ring Count
3
Aromatic Ring Count
2
cLogP
3.66
TPSA
46.01
Fraction CSP3
0.29
Chiral centers
0.0
Largest ring
6.0
QED
0.87
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Enzymes
Pathway
WNT signaling
Stem Cells
Cytoskeletal Signaling
Cell Cycle/DNA Damage
Epigenetics
Stem Cell/Wnt
Target
TNKS1, TNKS2
¦Â-catenin
Tankyrase-1
Tankyrase-2
TNKS1
TNKS2
??catenin
TNKS, TNKS2
TNKS inhibitor
β-catenin
PARP,Wnt/beta-catenin
TNKS, TNKS2, PARP1, PARP2
Primary Target
Tankyrase
MOA
Wnt/beta-catenin
Inhibitor
Tankyrase 1 (TNKS1) Inhibitors
Tankyrase 2 (TNKS2) Inhibitors
tankyrase inhibitor
Member status
member
Target subclass
PARP
PARP, PARP, PARP, PARP
Target class
Other post-translational modification
Other post-translational modification, Other post-translational modification, Other post-translational modification, Other post-translational modification
Orthogonal probe
AZ6102
Control
LDW643
Source data
