XAV-939

Catalog No.S1180 Batch:S118007

Technical Data

Formula

C₁₄H₁₁F₃N₂OS

Molecular Weight

312.31

CAS No.

284028-89-3

Solubility (25°C)*

In vitro

DMSO

12 mg/mL (38.42 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

4%DMSO 1 Corn oil

1.0mg/ml

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.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]

In vivo

AV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition.

Protocol (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[3]}	Animal Models Male Sprague-Dawley rats Dosages 3 mg/kg Administration i.p.

Cell Assay:^{^[1]}

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.

Animal Study:^{^[3]}

Animal Models
Male Sprague-Dawley rats
Dosages
3 mg/kg
Administration
i.p.

References

Customer Product Validation

: Data from [Data independently produced by Nat Commun, 2014, 5, 5455]

: Data from [Data independently produced by Dis Model Mech, 2014, 7(10), 1193-203]

: , , Cancer Lett, 2017, 400:194-202

: , , Dr. Marco Quarta of Stanford University

Selleck's XAV-939 has been cited by 392 publications

Double-Network DNA Macroporous Hydrogel Enables Aptamer-Directed Cell Recruitment to Accelerate Bone Healing [ Adv Sci (Weinh), 2024, 11(1):e2303637]	PubMed: 37949678
Activation of the Wnt/β-catenin signalling pathway enhances exosome production by hucMSCs and improves their capability to promote diabetic wound healing [ J Nanobiotechnology, 2024, 22(1):373]	PubMed: 38926800
RNF166 promotes colorectal cancer progression by recognizing and destabilizing poly-ADP-ribosylated angiomotins [ Cell Death Dis, 2024, 15(3):211]	PubMed: 38480683
The chromodomain protein CDYL confers forebrain identity to human cortical organoids by inhibiting neuronatin [ Cell Rep, 2024, 43(10):114814]	PubMed: 39378153
Pten regulates endocytic trafficking of cell adhesion and Wnt signaling molecules to pattern the retina [ Cell Rep, 2024, 43(4):114005]	PubMed: 38551961
Extraembryonic mesoderm cells derived from human embryonic stem cells rely on Wnt pathway activation [ Cell Prolif, 2024, 10.1111/cpr.13761]	PubMed: 39385268
SUMOylated Golgin45 associates with PML-NB to transcriptionally regulate lipid metabolism genes during heat shock stress [ Commun Biol, 2024, 7(1):532]	PubMed: 38710927
N6-methyladenosine-modified VGLL1 promotes ovarian cancer metastasis through high-mobility group AT-hook 1/Wnt/β-catenin signaling [ iScience, 2024, 27(3):109245]	PubMed: 38439973
Defining cis-regulatory elements and transcription factors that control human cortical interneuron development [ iScience, 2024, 27(6):109967]	PubMed: 38827400
S100A6 Regulates nucleus pulposus cell apoptosis via Wnt/β-catenin signaling pathway: an in vitro and in vivo study [ Mol Med, 2024, 30(1):87]	PubMed: 38877413

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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