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XAV-939

Name: XAV-939
Brand: Selleck Chemicals
SKU: S1180
Rating: 5 (402 reviews)

Synonyms: NVP-XAV939

Catalog No.S1180 Purity:99.95%

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

CAS No. 284028-89-3

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.

XAV-939 Related Products

Related Targets	PARP1 PARP2 PARP3 Tankyrase-1 Tankyrase-2 PARP14 PARP7 TNKS1 TNKS2	Click to Expand
Related Products	Veliparib (ABT-888) PJ34 HCl AG-14361 Iniparib (BSI-201) A-966492 G007-LK UPF 1069 AZD2461 Pamiparib ME0328 3-Aminobenzamide NMS-P118 Stenoparib (E7449) NVP-TNKS656 WIKI4 Benzamide BGP-15 2HCl NU1025 BYK204165 Fluzoparib (SHR-3162) Picolinamide	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library FDA-approved Drug Library Stem Cell Signaling Compound Library GPCR Compound Library Stem Cell Differentiation Compound Library	Click to Expand

Signaling Pathway

PARP Signaling Pathway

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

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 / c-Myc / cyclin D1 / E-cadherin / N-cadherin / Vimentin β-catenin / E-cadherin / N-cadherin		28177909
	Immunofluorescence	Hes1 / β-catenin / p-STAT3 Actin / PAR β-catenin / E-cadherin		25061499

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.

References

Chemical Information & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	4%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (3.20mM)	Taking the 1 mL working solution as an example, add 40 μL of 25 mg/ml clear DMSO stock solution to 960 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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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.

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