Home Stem Cells & Wnt PARP inhibitor - Wnt/beta-catenin inhibitor XAV-939 For research use only.

XAV-939

Synonyms: NVP-XAV939

XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.

XAV-939 Chemical Structure

XAV-939 Chemical Structure

CAS: 284028-89-3

Selleck's XAV-939 has been cited by 360 publications

Purity & Quality Control

Batch: Purity: 99.95%
99.95

Products often used together with XAV-939

SU5402

XAV-939 promotes anterior central nervous system identity, while SU5402 accelerates hPSC differentiation toward neuroectodermal lineages.

Chen S, Stem Cell Reports. 2018 Dec 11;11(6):1312-1323.

LDN-193189

XAV-939 and LDN-193189 are the least effective in improving the morphology of low-density P0 RPE cultures to varying extents.

Radeke MJ, et al. Genome Med. 2015 Jun 19;7(1):58.

SB431542

XAV-939 and SB431542 significantly suppress MSC gene expression.

Zhang Y, et al. Commun Biol. 2023 May 1;6(1):476.

ICG-001

XAV939 and ICG-001 decrease the proliferation of the IGROV1 and SKOV3 ovarian cancer cell lines.

Bocchicchio S, et al. J Cell Physiol. 2019 Dec;234(12):22130-22143.

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf-21 Kinase Assay 18.75 μM 60 min DMSO Inhibition of N-terminal GST-tagged TNKS2 expressed with IC50 of 0.0053 μM 23879431
HEK293T Function Assay DMSO Inhibition of Wnt signaling assessed as inhibition of forskolin-induced cAMP response element activation with IC50 of 0.078 μM 23879431
HEK293T Function Assay 10 μM DMSO Inhibition of beta-casein-dependent canonical Wnt3 pathway with IC50 of 0.051 μM 22191557
HEK293T Function Assay 24 h DMSO Inhibition of mouse Wnt3A signaling with IC50 of 0.078 μM 22260203
SW480 Function Assay 10 μM 24 h DMSO Stabilization of Axin2 with EC50 of 0.371 μM 22260203
HEK293T Function Assay 50 μM DMSO Has no Effect on forskolin-induced cAMP signaling in human HEK293T cells coexpressing CRE 22260203
IEC-6 Function Assay 6 h Antagonist activity at Beta-catenin/TCF assessed as inhibition of Wnt-3a-induced axin2 expression with IC50 of 0.64 μM 24060489
IEC-6 Function Assay 6 h Antagonist activity at Beta-catenin/TCF assessed as inhibition of Wnt-3a-induced lgr5 expression with IC50 of 2.9 μM 24060489
DLD1 Function Assay 20 μM 24 h DMSO Inhibition of tankyrase assessed as inhibition of TCF-dependent transcriptional activity 24527792
DLD1 Cytotoxic Assay 20 μM 10 d DMSO Cytotoxicity assessed as growth inhibition 24527792
VERO Function Assay 25 μM DMSO Disturbes PAR belt synthesis, affecting the actin cytoskeleton, cell shape and cell adhesion 25332845
HeLa Function Assay 10 μM 48 h Reduction of cytoplasmic distribution and nuclear translocation of β-catenin 25061499
SiHa Function Assay 10 μM 48 h Reduction of cytoplasmic distribution and nuclear translocation of β-catenin 25061499
HEK293 Function assay Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin, IC50 = 0.078 μM. 23844574
DLD1 Function assay 24 hrs Inhibition of tankyrase in human DLD1 cells assessed as reduction in Wnt activity after 24 hrs by TCF-luciferase reporter gene assay, IC50 = 0.707 μM. 25299683
Sf21 Function assay 2 hrs Inhibition of N-terminal GST-tagged human TNKS-2 (849 to 1166 residues) expressed in in insect sf21 cells preincubated for 2 hrs followed by substrate addition measured after 30 mins, IC50 = 0.017 μM. 27163581
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
A549 Growth inhibition assay 72 hrs Growth inhibition of human A549 cells after 72 hrs by MTT assay, IC50 = 12.3 μM. 29934219
Click to View More Cell Line Experimental Data

Biological Activity

Description XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.
Targets
TNKS2 [1]
(Cell-free assay)		 TNKS1 [1]
(Cell-free assay)
4 nM 11 nM
In vitro
In vitro

XAV-939 specifically inhibits tankyrase PARP activity. XAV-939 dramatically decreases DNA-PKcs protein levels, confirming the critical role of tankyrase poly-ADP-ribosylation activity in maintaining stability of the DNA-PKcs protein. The greatest reduction of DNA-PKcs protein levels (< 25% relative expression compared to DMSO treated controls) occurs at 12 hours with 1.0 μM XAV-939 exposure. Treatment of human lymphoblasts with 1.0 μM XAV-939 results in marked elevation of tankyrase 1 levels. [1]

XAV-939 is axin stabilizing agent. XAV-939 stimulates beta-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex. XAV-939 stabilizes axin by blocking the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2. Both tankyrase isoforms interact with a highly conserved domain of axin and stimulate its degradation through the ubiquitin-proteasome pathway. XAV-939 deregulates the Wnt/b-catenin pathway which has been implicated in many cancers. [2]
Cell Research Cell lines WTK1 lymphoblasts
Concentrations 1.0 μM
Incubation Time 8 hours
Method

XAV-939 is solubilized in DMSO at 55 °C to make a 10 mM stock solution which may be diluted later to a working concentration of 100 μM. WTK1 lymphoblasts treated with either DMSO or 1.0 μM XAV-939 for 8 hours are loaded into independent wells of a 4-20% gradient SDS-PAGE every 2 hours over the course of 6 hours. At each time point, DMSO and XAV-939 samples are loaded into wells immediately adjacent to the prior time point. The corresponding load times at 0, 2 and 4 hours results in total run times of 2, 4 and 6 hours respectively. The gel is analyzed via western blot for DNA-PKcs following completion of the final run time and is quantified after normalization to actin loading controls.
Experimental Result Images Methods Biomarkers Images PMID
Western blot β-catenin / E-cadherin / N-cadherin β-catenin / c-Myc / cyclin D1 / E-cadherin / N-cadherin / Vimentin 31060551
Immunofluorescence β-catenin / E-cadherin Actin / PAR Hes1 / β-catenin / p-STAT3 31060551
In Vivo
In vivo

AV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition.
Animal Research Animal Models Male Sprague-Dawley rats
Dosages 3 mg/kg
Administration i.p.

Chemical lnformation & Solubility

Molecular Weight 312.31 Formula

C14H11F3N2OS
CAS No. 284028-89-3 SDF Download XAV-939 SDF
Smiles C1CSCC2=C1N=C(NC2=O)C3=CC=C(C=C3)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 12 mg/mL ( (38.42 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
I want to inject XAV 939 (Cat # S1180) into mice through I.P. and just wonder what kind of solvent/solution I can use for this.

Answer:
S1180 XAV-939 can be dissolved in 4% DMSO+corn oil at 1 mg/ml as a clear solution. When preparing the solution, please dissolve the compound in DMSO clearly first. You can sonicate and warm it in water bath at about 45 degree to help dissolving. Then dilute with corn oil.

PARP Signaling Pathway Map

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