XAV939

• CAT Number: I002965
• CAS Number: 284028-89-3
• Molecular Formula: C₁₄H₁₁F₃N₂OS
• Molecular Weight: 312.31
• Purity: ≥95%
• Synonyms: 2-[4-(trifluoromethyl)phenyl]-1,5,7,8-tetrahydrothiopyrano[4,3-d]pyrimidin-4-one
• Target: Epigenetics
• Solubility: DMSO: ≤ 21.5 mg/mL
• Storage: 3 years -20C powder
• IC50: 11 nM(TNKS1); 4 nM(TNKS2)
• InChI: InChI=1S/C14H11F3N2OS/c15-14(16,17)9-3-1-8(2-4-9)12-18-11-5-6-21-7-10(11)13(20)19-12/h1-4H,5-7H2,(H,18,19,20)
• InChIKey: KLGQSVMIPOVQAX-UHFFFAOYSA-N
• SMILES: C1CSCC2=C1NC(=NC2=O)C3=CC=C(C=C3)C(F)(F)F

XAV939 is a small molecule and selective Wnt pathway β-catenin-mediated transcription inhibitor and axin stabilizing agent with IC50 of 11 and 4 nM for the inhibition of TNKS1 and TNKS2, respectively.

Reference

[1]. Huang SM et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature. 2009 Oct 1;461(7264):614-20.
[2]. Li Z, Yamauchi Y, Kamakura M, Murayama T, Goshima F, Kimura H, Nishiyama Y. ,Herpes simplex virus requires poly(ADP-ribose) polymerase activity for efficient replication and induces extracellular signal-related kinase-dependent phosphorylation and ICP0-dependent nuclear localization of tankyrase 1. J Virol. 2012 Jan;86(1):492-503. Epub 2011 Oct 19.
[3]. Kirby CA, Cheung A, Fazal A, Shultz MD, Stams T.,Structure of human tankyrase 1 in complex with small-molecule inhibitors PJ34 and XAV939.,Acta Crystallogr Sect F Struct Biol Cryst Commun. 2012 Feb 1;68(Pt 2):115-8. Epub 2012 Jan 21.
[4]. Ao A, Hao J, Hopkins CR, Hong CC.,DMH1, a Novel BMP Small Molecule Inhibitor, Increases Cardiomyocyte Progenitors and Promotes Cardiac Differentiation in Mouse Embryonic Stem Cells.,PLoS One. 2012;7(7):e41627. Epub 2012 Jul 27. bryonic Stem Cells. ,PLoS One. 2012;7(7):e41627. Epub 2012 Jul 27.
[5]. Chen HC, Zhu YT, Chen SY, Tseng SC.,Wnt signaling induces epithelial-mesenchymal transition with proliferation in ARPE-19 cells upon loss of contact inhibition.,Lab Invest. 2012 May;92(5):676-87.