4-[5-(3,4-DIMETHOXY-BENZYLIDENE)-4-OXO-2-THIOXO-THIAZOLIDIN-3-YL]-BUTYRIC ACID

Description

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.

Uses

iCRT5 is a selective CRT (β-catenin-responsive transcription) inhibitor.

References

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