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

KLF5:29 nM

ML264 强效抑制 DLD-1 细胞的活性（IC50 = 29 nM），最大效应高达 90% 以上。DLD-1 细胞是人类结直肠腺癌细胞。在亚μM剂量下，ML264 对其他细胞类型也有显著效应，包括 HCT116（人类结直肠癌细胞）、HT29（人类结直肠腺癌细胞）和 SW620（人类结直肠腺癌细胞）。对于 IEC-6 抗目标细胞（一种非转化的大鼠肠上皮细胞系）基本无影响，高剂量下的抑制率低于 50%[1]。该化合物通过改变细胞周期轮廓，在体外强效抑制 CRC 细胞的增殖[2]。

在一個已建立的結腸癌異種移植小鼠模型中，ML264於治療後五天內有效抑制腫瘤生長。這一效果是由於顯著降低細胞增殖所致，且ML264強效抑制KLF5及其轉錄激活因子EGR1的表達[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)