ML-264

ML-264 is a selective inhibitor of Krüppel-like factor 5 (KLF5), a zinc finger-containing transcription factor that is highly expressed in rapidly dividing intestinal epithelial cells. It displays an IC₅₀ value of 29 nM in a cell-based assay for proliferation of KLF5-expressing DLD-1 cells and an IC₅₀ value of 81 nM in a cell-based luciferase assay but does not inhibit kinases associated with the KLF5 pathway, as determined using a panel of 47 selected kinases.¹ ML-264 induces death in most colon cancer cell lines (HCT116, IC₅₀ = 560 nM; HT-29, IC₅₀ = 130 nM; SW620, IC₅₀ = 430 nM), with cytotoxicity toward an established xenograft mouse model of colon cancer as well.^1,2

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1. Bialkowska, A., Crisp, M., Maddoux, F., et al. ML264: An antitumor agent that potently and selectively inhibits krüppel-like factor five (KLF5) expression: A probe for studying colon cancer development and progression. Probe Reports from the NIH Molecular Libraries Program (2011).

2. de Sabando, A.R., Wang, C., He, Y., et al. ML264, a novel small-molecule compound that potently inhibits growth of colorectal cancer. Mol. Cancer Ther. 15(1), 72-83 (2016).