SR18662 is an optimized compund based on ML264 that inhibits Krüppel-like factor 5 (KLF5) with IC50 of 4.4 nM. SR18662 reduces the viability of multiple colorectal cancer cell lines. SR18662 induces apoptosis.
Treatment with SR18662 significantly reduces growth and proliferation of CRC cells. SR18662 shows improved efficacy in reducing viability of multiple CRC cell lines. Flow cytometry analysis following SR18662 treatment shows an increase in cells captured in either S or G2/M phases of the cell cycle and a significant increase in the number of apoptotic cells. SR18662 treatment also reduces the expression of cyclins and components of MAPK and WNT signaling pathways.[1]
A significant dose-dependent inhibition of xenograft growth in mice is observed following SR18662 treatment that exceeds the effect of ML264 at equivalent doses. SR18662 is potential for colorectal cancer therapy.[1]
[1] Julie Kim, et al. Mol Cancer Ther. 2019 Nov;18(11):1973-1984.