XAV-939

Catalog No.S1180 Batch:S118002

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Technical Data

Formula

C14H11F3N2OS
Molecular Weight 312.31 CAS No. 284028-89-3
Solubility (25°C)* In vitro DMSO 62.5 mg/mL (200.12 mM)
Water Insoluble
Ethanol Insoluble
* <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.

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 405 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
GPA33 expression in colorectal cancer can be induced by WNT inhibition and targeted by cellular therapy [ Oncogene, 2024, ] PubMed: 39472498
Cpt1a Drives primed-to-naïve pluripotency transition through lipid remodeling [ Commun Biol, 2024, 7(1):1223] PubMed: 39349670
Deficiencies in corin and atrial natriuretic peptide-mediated signaling impair endochondral ossification in bone development [ Commun Biol, 2024, 7(1):1380] PubMed: 39443661
SUMOylated Golgin45 associates with PML-NB to transcriptionally regulate lipid metabolism genes during heat shock stress [ Commun Biol, 2024, 7(1):532] PubMed: 38710927

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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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