8-(2-Ethoxyphenyl)-7,8-dihydro-1,3-Dioxolo[4,5-g]quinolin-6(5H)-one

Description

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.

References

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