ML264 ML264 (CID-51003603), a selectively inhibitor of kruppel-like factor 5 (KLF5) ,potently Inhibits Growth of Colorectal Cancer.
Targets
KLF5 (Cell-based assay for proliferation of DLD-1 cells) 29 nM
In vitro
ML264 potently halts DLD-1 viability (IC50 = 29 nM) with high maximal effect (>90%). DLD-1 cells are human colorectal adenocarcinoma cells. ML264 has significant effects at submicromolar doses on other cell types as well, including HCT116 (human colorectal carcinoma), HT29 (human colorectal adenocarcinoma), and SW620 (human colorectal adenocarcinoma). The IEC-6 anti-target (a nontransformed rat intestinal epithelial cell line) is largely unaffected, with inhibition below 50% at the highest dose.This compound potently inhibits proliferation of CRC cells in vitro through modifications of the cell cycle profile.
In vivo
In an established xenograft mouse model of colon cancer, ML264 efficiently inhibits growth of the tumor within five days of treatment. this effect is caused by a significant reduction in proliferation and that ML264 potently inhibits the expression of KLF5 and EGR1, a transcriptional activator of KLF5.
Cell Research(from reference)
Cell lines：DLD-1 and HCT116 colorectal cancer cell lines
