FQI1 (599151-35-6) is an inhibitor of transcription factor LSF specifically targeting its DNA binding and corresponding transcriptional activity (IC50=2.1 μM). Rapidly induces apoptosis in an aggressive hepatocellular carcinoma (HCC) cell line and dramatically inhibits tumor growth in a mouse xenograft model with no general tissue cytotoxicity.1,2 In human HCC cells, FQI1 induced mitotic arrest with an accompanying increase in cyclin B1.3 Blocks LSF-stimulated activation of DNA methyltransferase 1.4 Cell permeable.
1) Grant et al. (2012), Antiproliferative small-molecule inhibitors of transcription factor LSF reveal oncogene addiction to LSF in hepatocellular carcinoma; Proc. Natl. Acad. Sci. USA, 109 4503
2) Santhekadur et al. (2012), The transcription factor LSF: a novel oncogene for hepatocellular carcinoma; Am. J. Cancer Res., 2 269
3) Raiasekaran et al. (2015), Small molecule inhibitors of Late SV40 Factor (LSF) abrogate hepatocellular carcinoma (HCC): Evaluation using an endogenous HCC model; Oncotarget 6 26266
4) Chin et al. (2016), Transcription factor LSF-DNMT1 complex dissociation by FQI1 leads to aberrant DNA methylation and gene expression; Oncotarget, 7 83627