XAV-939

Name: XAV-939
Brand: MedChemExpress
SKU: HY-15147
Rating: 5.0 (142 reviews)

Cat. No.: HY-15147 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

XAV-939 Chemical Structure

CAS No. : 284028-89-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 72	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 216	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 336	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 600	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 142 publication(s) in Google Scholar

Other Forms of XAV-939:

XAV-939 (GMP) Get quote

130 Publications Citing Use of MCE XAV-939

: XAV-939 purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2023 Apr 20;e17101. [Abstract]; XAV939 (20 μM; 3 days) restores the expression of Homer1, PSD95, and GluR1 in Shank3 knockout (KO) human neurons.

: XAV-939 purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2022 Dec 12;249:114410. [Abstract]; XAV-939 (5 μM) significantly decreases the expression level of β-catenin in A549 cells.

: XAV-939 purchased from MedChemExpress. Usage Cited in: Am J Physiol Renal Physiol. 2020 Sep 1;319(3):F458-F468. [Abstract]; Representative Western blot showing FN protein abundance in HMCs cultured in media containing NG or HG in the absence or presence of liraglutide (100 nM) or DMSO (1:1000) or XAV-939 (5 μM) for 24 h.

: XAV-939 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 18;9(2):27. [Abstract]; The cellular locations of β-catenin are detected by western blot. GAPDH, Histone H3, and ATP1A1 are used to normalize protein expression in total lysates and nuclear and membrane fractions, respectively. SGC-7901 cells with PCDHGA9 overexpression or vector control cells are grown in media with or without 10 μg/mL inhibitor of β-catenin (XAV-939).

: XAV-939 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jun 21;9:660. [Abstract]; By Western blotting, the α-SMA and palladin proteins are determined in cells that are pretreated with NF-κB (JSH-23), Wnt/β-catenin (XAV939), EGFR (CP-358774), p38 MAPK (TAK-715), and Smad3 (SIS3) inhibitors and are followed by TWEAK stimulation.

: XAV-939 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):2061-2067. [Abstract]; Western blot analysis and alizarin red staining of hDFSCs transfected by EZH2-siRNA and treated by XAV-939. DMSO is used as a vehicle control.

: XAV-939 purchased from MedChemExpress. Usage Cited in: Anticancer Drugs. 2018 Mar;29(3):208-215. [Abstract]; SUM159 sphereforming cells are treated with 15 μM XAV-939 for 7 days, and the protein expression levels of breast cancer stem cells (CSCs) markers are detected by western blotting.

: XAV-939 purchased from MedChemExpress. Usage Cited in: Anticancer Drugs. 2018 Mar;29(3):208-215. [Abstract]; SUM159 sphere-forming cells are treated with GDC-0449 (15 μM), a Smoothened (Smo) inhibitor for 7 days, and the protein expression levels of breast cancer stem cells (CSCs) play markers are detected by western blotting.

: XAV-939 purchased from MedChemExpress. Usage Cited in: Biomed Res Int. 2017;2017:1972608. [Abstract]; To investigate the roles of β-catenin, XAV939 (β-catenin inhibitor) was added to MNT group. Total protein is used to observe the expression of Nrf2 and LC3.

: XAV-939 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2016 Mar 29;113(13):E1898-906. [Abstract]; Analysis of the in vitro role of the Wnt/β–catenin pathway in the regulation of AQP2 expression in response to sPRR-His treatment. Effect of XAV on sPRR-His-induced AQP2 expression (n = 6 per group).

: XAV-939 purchased from MedChemExpress. Usage Cited in: Comp Biochem Phys B. 2016 Jan;191:155-62. [Abstract]; The protein expression of Wnt10b and p-GSK-3β is significantly induced by LiCl treatment (A and B). Nevertheless, XAV939 treatment significantly inhibits the protein expression of p-GSK-3β (B). Moreover, the protein expression of p-β-catenin is significantly inhibited by LiCl treatment, but significantly induced by XAV939 treatment (C).

: XAV-939 purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2016;39(1):360-70. [Abstract]; EGF upregulates the expression of follicle-regulatory genes via Wnt/β-catenin signaling pathway. (A) The mRNA and (B, C) the protein levels of Survivin, Msx2 and SGK3 in the ORS cells with EGF treatment/overexpression and/or XAV-939 treatment.

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View All Isoforms

PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[6]

TNKS2

2 nM (IC₅₀)

TNKS1

5 nM (IC₅₀)

ARTD2

479 nM (IC₅₀)

ARTD1

5500 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	12.3 μM Compound: XAV939	Growth inhibition of human A549 cells after 72 hrs by MTT assay Growth inhibition of human A549 cells after 72 hrs by MTT assay	[PMID: 29934219]
COLO 320DM	GI₅₀	17 μM Compound: XAV939	Antiproliferative activity against human COLO320DM cells assessed as inhibition of cell growth measured after 4 days by CellTiter-Glo assay Antiproliferative activity against human COLO320DM cells assessed as inhibition of cell growth measured after 4 days by CellTiter-Glo assay	[PMID: 30883102]
DLD-1	IC₅₀	0.707 μM Compound: 1, XAV-939	Inhibition of tankyrase in human DLD1 cells assessed as reduction in Wnt activity after 24 hrs by TCF-luciferase reporter gene assay Inhibition of tankyrase in human DLD1 cells assessed as reduction in Wnt activity after 24 hrs by TCF-luciferase reporter gene assay	[PMID: 25299683]
HEK293	IC₅₀	0.078 μM Compound: 1, XAV939	Inhibition of mouse Wnt3A signaling in human HEK293 cells after 1 day by super top flash luciferase reporter gene assay Inhibition of mouse Wnt3A signaling in human HEK293 cells after 1 day by super top flash luciferase reporter gene assay	[PMID: 22260203]
HEK293	IC₅₀	0.078 μM Compound: 1, XAV939	Inhibition of Wnt signaling in human HEK293 cells assessed as inhibition of forskolin-induced cAMP response element activation by STF luciferase reporter gene assay Inhibition of Wnt signaling in human HEK293 cells assessed as inhibition of forskolin-induced cAMP response element activation by STF luciferase reporter gene assay	[PMID: 23879431]
HEK293	IC₅₀	0.078 μM Compound: 1, XAV939	Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin	[PMID: 23844574]
HEK293	IC₅₀	272 μM Compound: 3, XAV939	Inhibition of Tankyrase in human HEK293 cells assessed as inhibition of Wnt pathway by Wnt3a-induced STF assay Inhibition of Tankyrase in human HEK293 cells assessed as inhibition of Wnt pathway by Wnt3a-induced STF assay	[PMID: 23316926]
HEK-293T	IC₅₀	51 nM Compound: 2, XAV939	Inhibition of beta-casein-dependent canonical Wnt3 pathway in human HEK293T cells by luciferase reporter gene assay Inhibition of beta-casein-dependent canonical Wnt3 pathway in human HEK293T cells by luciferase reporter gene assay	[PMID: 22191557]
Sf21	IC₅₀	0.0053 μM Compound: 1, XAV939	Inhibition of N-terminal GST-tagged TNKS2 (unknown origin) expressed in baculovirus infected sf21 cells after 60 mins by LC-MS analysis Inhibition of N-terminal GST-tagged TNKS2 (unknown origin) expressed in baculovirus infected sf21 cells after 60 mins by LC-MS analysis	[PMID: 23879431]
Sf21	IC₅₀	17 nM Compound: 5; XAV939	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 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	[PMID: 27163581]
Sf9	IC₅₀	2.1 nM Compound: XAV939	Inhibition of human N-terminal GST-tagged TNKS2 (667 to 1166 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay Inhibition of human N-terminal GST-tagged TNKS2 (667 to 1166 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay	[PMID: 31042381]
Sf9	IC₅₀	4.2 nM Compound: XAV939	Inhibition of human N-terminal GST-tagged TNKS1 (1001 to 1327 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay Inhibition of human N-terminal GST-tagged TNKS1 (1001 to 1327 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay	[PMID: 31042381]
SW480	GI₅₀	> 50 μM Compound: XAV939	Growth inhibition of human SW480 cells by Cell-titer-fluor reagent based assay Growth inhibition of human SW480 cells by Cell-titer-fluor reagent based assay	[PMID: 31769984]
SW480	EC₅₀	0.371 μM Compound: 1, XAV939	Stabilization of Axin2 in human SW480 cells after 24 hrs by sandwich ELISA Stabilization of Axin2 in human SW480 cells after 24 hrs by sandwich ELISA	[PMID: 22260203]

In Vitro

XAV-939 has activity against TNKS1 and TNKS2 with IC₅₀ values of 5 nM and 2 nM, respectively^[1].
XAV-939 (0.3-30 μM; 3 or 10 days) enhances osteoblast differentiation of hBMSCs^[2].
XAV-939 (3 μM) promotes osteoblast differentiation of hMSCs via accumulation of SH3BP2^[2].
XAV-939 (3 μM; 10 days) upregulates the expression of OPG and downregulates the expression of RANKL in hBMSCs during osteoblast differentiation^[2].
XAV-939 suppresses Wnt/β-catenin signaling and promotes SFRP3 and SFRP4 expression^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

Cell Line:	hMSC-TERT cell line
Concentration:	0.3, 3, and 30 μM
Incubation Time:	3 days
Result:	Showed no significant effect on proliferation at day 1, 2, and 3 at dose of 0.3 and 3 μM but inhibited hMSCs cell proliferation on day 3 at dose of 30 μM.

Apoptosis Analysis^[2]

Cell Line:	hMSC-TERT cell line
Concentration:	3 µM
Incubation Time:	3 days
Result:	Showed a minute percentage of cell death (apoptosis and necrosis) in the XAV-939-treated hBMSC

RT-PCR^[2]

Cell Line:	hMSC-TERT cell line
Concentration:	3 µM
Incubation Time:	10 days
Result:	Upregulated gene expression of osteoblast-associated gene markers including: ALP, COL1A1, RUNX2, and OC.

In Vivo

XAV-939 rescues mechanical stress-induced cartilage degeneration in vivo^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

312.31

Formula

C₁₄H₁₁F₃N₂OS

CAS No.

284028-89-3

Appearance

Solid

Color

White to off-white

SMILES

O=C1C(CSCC2)=C2N=C(C3=CC=C(C(F)(F)F)C=C3)N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 15.62 mg/mL (50.01 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.2019 mL	16.0097 mL	32.0195 mL
5 mM	0.6404 mL	3.2019 mL	6.4039 mL
10 mM	0.3202 mL	1.6010 mL	3.2019 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 1.56 mg/mL (5.00 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.56 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.6 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1.56 mg/mL (5.00 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.56 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.6 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 1.56 mg/mL (5.00 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 1.56 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.6 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (16.01 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.91%

Select Batch:

Data Sheet (279 KB) SDS (420 KB)

COA (247 KB) HNMR (273 KB) LCMS (264 KB) Elemental Analysis Report (106 KB)

Handling Instructions (2659 KB)

References

[1]. Mohit Narwal, et al. Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity. J Med Chem. 2013 Oct 24;56(20):7880-9. [Content Brief]

[2]. Nuha Almasoud, et al. Tankyrase inhibitor XAV-939 enhances osteoblastogenesis and mineralization of human skeletal (mesenchymal) stem cells. Sci Rep. 2020 Oct 7;10(1):16746. [Content Brief]

[3]. Senxin Cai, et al. Mechanical stress reduces secreted frizzled-related protein expression and promotes temporomandibular joint osteoarthritis via Wnt/β-catenin signaling. Bone. 2022 Aug;161:116445. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.2019 mL	16.0097 mL	32.0195 mL	80.0487 mL
	5 mM	0.6404 mL	3.2019 mL	6.4039 mL	16.0097 mL
	10 mM	0.3202 mL	1.6010 mL	3.2019 mL	8.0049 mL
	15 mM	0.2135 mL	1.0673 mL	2.1346 mL	5.3366 mL
	20 mM	0.1601 mL	0.8005 mL	1.6010 mL	4.0024 mL
	25 mM	0.1281 mL	0.6404 mL	1.2808 mL	3.2019 mL
	30 mM	0.1067 mL	0.5337 mL	1.0673 mL	2.6683 mL
	40 mM	0.0800 mL	0.4002 mL	0.8005 mL	2.0012 mL
	50 mM	0.0640 mL	0.3202 mL	0.6404 mL	1.6010 mL

XAV-939 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

XAV-939284028-89-3XAV939XAV 939β-cateninPARPBeta cateninpoly ADP ribose polymeraseTankyraseTNKS1TNKS2hMSCsWnt signalingcancerfibrotic diseaselow bone formationInhibitorinhibitorinhibit

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XAV-939

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Other Forms of XAV-939:

XAV-939 Related Antibodies

130 Publications Citing Use of MCE XAV-939

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Purity & Documentation

References

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XAV-939 Related Antibodies

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Complete Stock Solution Preparation Table

XAV-939 Related Classifications

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