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
15
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
DESCRIPTION
XAV-939 is a Tankyrase inhibitor. XAV-939 has inhibitory activity for TNKS1 and TNKS2 with IC50 values of 5 nM and 2 nM, respectively. XAV-939 also is an enhancer of osteoblastic differentiation of hMSCs. XAV-939 can be used for the research of conditions associated with activated Wnt signaling, such as cancer, fibrotic diseases and conditions associated with low bone formation[1][2][3].
PRICE
50
DESCRIPTION
XAV-939 (NVP-XAV939) is a Tankyrase (TNKS) inhibitor that inhibits TNKS1 and TNKS2 (IC50=11/4 nM). XAV-939 selectively inhibits Wnt/??-catenin-mediated transcription.
MOA
Inhibitor
(Chemical Probes.org)
DESCRIPTION
Endothelial lipase and lipoprotein lipase inhibitor
(Tocris Bioactive Compound Library)
DESCRIPTION
Tankyrase inhibitor; inhibits wnt signaling
(Tocriscreen Total)
DESCRIPTION
Potent tankyrase inhibitor
(Tocriscreen Plus)
DESCRIPTION
XAV-939 is a potent tankyrase inhibitor that targets Wnt/β-catenin signaling. XAV-939 inhibits tankyrase 1 and tankyrase 2 with IC50s of 10 and 4 nM, respectively.
(Enamine Bioactive Compounds)
DESCRIPTION
XAV-939 (NVP-XAV939) is a Tankyrase (TNKS) inhibitor that inhibits TNKS1 and TNKS2 (IC50=11/4 nM). XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
2
Organisms
0
Compound Sets
21
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
Chemical Probes.org
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
Enamine Bioactive Compounds
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics 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
29
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
Chromatin/Epigenetic
Cytoskeletal Signaling
DNA Damage/DNA Repair
Stem Cells
Cell Cycle/DNA Damage
Epigenetics
Stem Cell/Wnt
Target
TNKS1, TNKS2
¦Â-catenin
Tankyrase-1
Tankyrase-2
PARP
TNKS1
TNKS2
β-catenin
??catenin
TNKS, TNKS2
TNKS inhibitor
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 class
Other post-translational modification
Other post-translational modification, Other post-translational modification, Other post-translational modification, Other post-translational modification
Orthogonal probe
AZ6102
Target subclass
PARP, PARP, PARP, PARP
Control
LDW643
Recommended Cell Concentration
None
Source data
