ML264 (CID-51003603) is a selective kruppel-like factor 5 (KLF5) inhibitor, which potently Inhibits growth of Colorectal Cancer.

KLF5:29 nM

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[1].This compound potently inhibits proliferation of CRC cells in vitro through modifications of the cell cycle profile[2].

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[2].

For cell proliferation experiments, DLD-1 and HCT116 cells are treated with 10μM ML264 or with vehicle (DMSO). Live cells are collected at 24, 48 and 72 hours post treatment and their numbers are determined by counting using a Coulter counter; In MTS assay, DLD-1 and HCT116 cells are treated with 10μM ML264 or with vehicle (DMSO). After 24, 48, and 72 hours of incubations, 20 μL of MTS solution  is added to each well and an analysis is performed according to the manufacturer's protocol. (Only for Reference)