| References: |
ML-264 is a Krüppel-like factor 5 (KLF5) inhibitor That Potently Inhibits Growth of Colorectal Cancer. ML264 is highly active (IC50 = 29 nM is a cell-based assay for proliferation of DLD-1 cells, IC50 = 81 nM in a cell-based luciferase assay). It lacks cytotoxicity in the IEC-6 control cell line (IC50 >50 μM, <50% inhibition was observed at 100 μM). Robust activity was also seen in several other KLF5-expressing cell types as well (e.g., HCT116, IC50 = 560 nM; HT29, IC50 = 130 nM; SW620, IC50 = 430 nM). ML264 is a good candidate for in vivo anticancer studies, with great potential for use in long time-course in situ studies aimed to elucidate the role of KLF5 as a regulator of cellular proliferation and tumor formation in the intestinal epithelium. |
