[CAS NO. 1550008-55-3]  ML264

ML264 is highly active (IC ₅₀ =29 nM is a cell-based assay for proliferation of DLD-1 cells, IC ₅₀ =81 nM in a cell-based luciferase assay). ML264 lacks cytotoxicity in the IEC-6 control cell line (IC ₅₀ >50 μM, <50% inhibition is observed at 100 μM). Robust activity is also seen in several other KLF5-expressing cell types as well (e.g., HCT116, IC ₅₀ =560 nM; HT29, IC ₅₀ =130 nM; SW620, IC ₅₀ =430 nM). Western blot analysis shows that ML264 significantly reduces KLF5 expression ^[1] . The effects of ML264 are tested on the rate of cell proliferation of colon cancer cells lines DLD-1 and HCT116 over 72 hours. ML264 efficiently inhibits the rate of proliferation of both cell lines. A significant decrease in proliferation is evident within 24 hours of treatment and by 72 hours the live cell numbers of ML264-treated and vehicle-treated cells differed by 15- to 30- fold. An MTS assay that allows the quantification of metabolically active cells is performed. ML264 treatment significantly reduces the number of cells undergoing mitosis in DLD-1 cells at 24, 48 and 72 hours ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.