iCRT5 (18623-44-4) is a selective CRT (β-catenin-responsive transcription) inhibitor.¹  IC50=18 nM for Wnt responsive STF16 luciferase. Acts via interfering with the β-catenin, TCF4 interaction.¹ Displays poor inhibition of cell proliferation in triple-negative breast cancer cells.² Increases the surface expression of MHCII, CD80 and CD86 on unstimulated dendritic cells (DCs) with no detrimental effects on immune-phenotype of stimulated DCs.³ Modulators of Wnt signaling show great promise in animal models of several cancers.⁴ Cell permeable.

References/Citations:

1) Gonsalves et al. (2011), An RNAi-based chemical genetic screen identifies three small-molecule inhibitors of the Wnt/wingless signaling pathway; Proc. Natl. Acad. Sci. USA, 108 5954
2) Bilir et al. (2013), Wnt signaling blockage inhibits cell proliferation and migration, and induces apoptosis in triple-negative breast cancer cells; J. Transl. Med., 11 280
3) Kafer et al. (2016), Inhibitors of β-catenin affect the immune-phenotype and functions of dendritic cells in an inhibitor-specific manner; Immunopharmacol., 32 118
4) Anastas et al. (2013), WNT signaling pathways as therapeutic targets in cancer; Nat. Rev. Cancer, 13 11