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 (Cat No.: I002965) is a small molecule inhibitor primarily used in research to block the Wnt/β-catenin signaling pathway, which plays a critical role in cell growth, differentiation, and cancer progression. By inhibiting tankyrase enzymes, XAV939 prevents the stabilization of β-catenin, thereby suppressing the Wnt signaling pathway. This compound has shown potential in cancer research, particularly in targeting cancers with dysregulated Wnt signaling, and is also being explored for its therapeutic potential in diseases like colorectal cancer and other Wnt-related disorders.

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.