KYA-1797K is a derivative of KY1220 with improved inhibitory activity for Wnt/β-catenin signaling.
KYA-1797K dose-dependently decreases Wnt3a-CM-induced TOPflash reporter activation with IC50 of 0.75 uM.
KYA-1797K is more effectively reduces the levels of both β-catenin and pan-Ras as well as the activities of ERK and Akt in SW480 cells.
KYA-1797K binds to Axin (Kd to WT axin-RGS=0.29 uM) and destabilizes b-catenin and Ras; inhibits growth of CRC cells with GI50 of 4-5 uM.
KYA-1797K suppresses the tumors induced by APC and KRAS mutations in tumor xenograft mice (25 mg/kg, i.p.).
