Fig. 1.

HI-B1 is a small molecule that preferentially kills cancer cells in which β-catenin is critical for survival.

(a) Chemical structure of HI-B1.

(b) DLD1 (left panel) and CACO2 (right panel) cells were transfected with TOPFlash, which contains TCF4 binding sequences, or FOPFlash (as a negative control) and then treated with different doses of HI-B1 for 24 h. Firefly luciferase activity was normalized with Renilla luciferase activity.

(c) Cells were treated with HI-B1 at different doses for 48 h and then viability was assessed by MTS assay.

(d) Lysates of nine different cell lines were prepared and β-catenin expression was detected by western blots.

(e) Cells were incubated for 48 h after the shRNA infection and antibiotic selection. Apoptosis was measured by annexin V/propidium iodide staining and flow cytometry.

(f) DLD1, CACO2, HCT116, H838 and CCD-18Co cell lines were treated with HI-B1. Apoptosis was measured after 48 h of treatment with flow cytometry.

All values of graphs present mean ± standard deviation (SD) (in triplicate). Significant differences were calculated by one-way ANOVA compared with DMSO-treated group or sh-mock group (*P < 0.05, **P < 0.01, ***P < 0.001).