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XAV-939

Cat. No.
: NU09018
Synonyms
: 2-[4-(trifluoromethyl)phenyl]-7,8-dihydro-5H-thiino[4,3-d]pyrimidin-4-ol
CAS No.
: 284028-89-3
Formula
: C14H11F3N2OS (312.3)
Appearance
: Off-white powder
Purity
: 98% or more (HPLC), NMR (Conforms) 
Solubilization
: May be dissolved in DMSO (25 mg/ml)
Storage
: Store as supplied at room temperature for up to 2 years. Store solutions at -20°C for up to 2 months.
Pharmacology
:  Tankyrase inhibitor (IC50=11 and 4 nM for TNKS1 and 2 respectively). Antagonizes Wnt signaling downstream of receptor activation via stabilization of axin, a negative regulator of β-catenin1. Robustly induces cardiomyogenesis of stem cells2.
Reduces experimental fibrosis in a mouse model of bleomycin-induced dermal fibrosis3. Promotes apoptosis in a neuroblastoma cell line via telomere shortening4. An important tool for probing the activation of the Wnt/β-catenin pathway in cells5. Cell permeable.
References
: 1. S. Huang et al. Nature 2009 46:614
  2. H Wang et al. ACS Chem. Biol. 2011 6:192
  3. A Distler Wang et al. Ann. Rheum. Dis. 2013 72:1575
  4. X Tian et al. Oncol. Rep. 2014 32:1999
  5. KC Davidson et al. Proc. Natl. Acad. Sci. USA 2012 109:4485

 

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