Supplementary Fig S1-S5 from The Discovery and Characterization of K-756, a Novel Wnt/β-Catenin Pathway Inhibitor Targeting Tankyrase

Abstract

<p>Supplementary Fig. S1: A, CTNNB1 siRNAs suppress the target gene and B, the target protein. C, CTNNB1 siRNAs inhibit reporter activity and D, change the expression of Wnt/β-catenin downstream genes.; Supplementary Fig. S2: A, K-756 does not inhibit cell growth of DLD-1/TCF-Luc cells. B, CTNNB1 siRNAs suppress the target gene in COLO 320DM and SW403 cells. C, K-050, and inactive analogue of K-756, does not inhibit COLO 320DM cells.; Supplementary Fig. S3: A, XAV939 and B, IWR-1 stabilize Axins and suppress active β-catenin in COLO 320DM and SW403 cells. C, The Axin stabilization and active β-catenin levels are higher in K-756-treated cells than XAV939-treated cells.; Supplementary Fig. S4: A, PK data of K-756. B, LGR5 inhibition by K-756 in in vitro. Time course PD experiments of C, FGF20, D, LGR5 and E, reporter activity in tumors of K-756-administered mice.; Supplementary Fig. S5: A, Axin and active β-catenin expression in K-756-treated PC-9 and NCI-H322 cells. B, The expression change of Wnt/β-catenin downstream gene in K-756-treated NCI-H322 cells.</p>