CWP232228 is such an inhibitor, which was reported to induce apoptosis and cell cycle arrest in HCT116 cells,380 also to show effects on liver and breast CSCs.381,382 LF3, a 4-thioureido-benzenesulfonamide derivative, reduced tumor growth and induced differentiation in a CRC xenograft murine model.383 Moreover, BC2059, an anthraquinone oxime-analog repressing Lef1/Tcf4 activity, was elucidated to induce the apoptosis of HL-60, HEL, and K562 significantly.384,385 BC2059 is currently testified in a phase I clinical trial of desmoid tumor (Table 2). The gene discussed is LEF1; the disease is colorectal carcinoma.