KY1220 is a small molecule destabilizer of both β-catenin and Ras via inhibition of the Wnt/β-catenin pathway (IC50=2.1 uM).
KY1220 dose-dependently decreases Wnt3a-CM-induced TOPflash reporter activation and mRNA expression of Wnt target genes CCND1 and MYC in HEK293 cells.
KY1220 reduces β-catenin and pan-Ras protein levels via polyubiquitin-dependent proteasomal degradation, consequently inhibits the activities of both ERK and Akt in various CRC cell lines.
KY1220 efficiently inhibits proliferation and transformation in HCT15, SW480, D-WT and D-MT CRC cells.
