Name: XAV-939
Price: 180.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    XAV-939 is a small-molecule inhibitor of tankyrase 1/2 with IC50 values of 4 and 11 nM, respectively [1].
    XAV-939 was screened out as an inhibitor of Wnt/β-catenin pathway. In HEK293 cells, XAV-939 significantly inhibited the Wnt3a-stimulated STF activity and β-catenin accumulation. In SW480 cells, XAV-939 also inhibited STF activity and increased β-catenin phosphorylation. XAV-939 was demonstrated to stabilize the axin levels through inhibiting tankyrases and subsequently inhibit the Wnt signaling. It tightly bound to the catalytic domains of tankyrase 1 and tankyrase 2 with Kd values of 99 and 93 nM, respectively. In addition, XAV-939 significantly inhibited colony formation of β-catenin-dependent DLD-1 cells but not β-catenin-independent RKO cells [1].
    
    [1] Huang S M A, Mishina Y M, Liu S, et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature, 2009, 461 (7264): 614-620.
- Properties
  - Alternative Name
    
    2-[4-(trifluoromethyl)phenyl]-1,5,7,8-tetrahydrothiopyrano[4,3-d]pyrimidin-4-one
    
    CAS Number
    
    284028-89-3
    
    Molecular Formula
    
    C14H11F3N2OS
    
    Molecular Weight
    
    312.31
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥15.62 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Shan Lin, Qingui Chen, et al."Overexpression of HOXB4 Promotes Protection of Bone Marrow Mesenchymal Stem Cells Against Lipopolysaccharide-Induced Acute Lung Injury Partially Through the Activation of Wnt/β-Catenin Signaling." J Inflamm Res. 2021 Jul 27;14:3637-3649. PMID:34349541
    2. Grunewald ME, Chen Y, et al. "The coronavirus macrodomain is required to prevent PARP-mediated inhibition of virus replication and enhancement of IFN expression." PLoS Pathog. 2019 May 16;15(5):e1007756. PMID:31095648
    3. Jia J, Qiao Y, et al."Tankyrase inhibitors suppress hepatocellular carcinoma cell growth via modulating the Hippo cascade." PLoS One. 2017 Sep 6;12(9):e0184068. PMID:28877210

XAV-939

XAV-939

Background

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