Catalog No.S1180 Synonyms: NVP-XAV939
Molecular Weight(MW): 312.31
XAV-939 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.
Cited by 21 Publications
5 Customer Reviews
Fluorescence microscopy of pSuper or Cdo shRNA expressing P19 cells at ITS1 immunostained withβ-tubulin III antibodies. Size bar=100 um. P19/control or P19/Cdo shRNA cells were treated with DMSO or XAV939 in the differentiation medium for 72 h followed by immunostaining.
Nat Commun 2014 5, 5455. XAV-939 purchased from Selleck.
Cells plated at 2 x 104 in 24 multiwell with DMEM 10% FBS preconditioning 24 hrs (pretreatment without wnt) switch medium from 2% HS + WNT 100 ng/ml
Dr. Marco Quarta of Stanford University. XAV-939 purchased from Selleck.
Fig. 1. Canonical Wnt Signaling Inhibits Prostatic Bud Number Similar to TCDD. E14.5 male UGSs were cultured for 4 days in media containing 10 nM DHT with either vehicle 1 nM TCDD; recombinant DKK1 + DKK2 (500 ng/ml each); or 10 μM XAV-939 to inhibit canonical Wnt signaling. Buds were visualized by performing IHC specific for ecadherin, an epithelium marker (green). The number of prostatic buds was determined by confocal microscopy. Yellow arrowheads indicate areas where buds are present. U indicates urethra. Results are mean ±SE for at least four litter-independent samples per treatment. Asterisk indicates a significant decrease compared to control p < 0.05.
XAV-939 purchased from Selleck.
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|Description||XAV-939 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 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.  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. 
|In vitro||DMSO||12 mg/mL (38.42 mM)|
|In vivo||30% PEG 400+0.5% Tween 80+5% Propylene glycol||30mg/mL|
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