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Description

A cell-permeable dihydroquinolinone compound that acts as a potent, specific, and reversible inhibitor of DNA-binding activity of Late SV40 Factor (LSF) and blocks LSF transactivation (IC50 = 2.1 µ,M in NIH 3T3 cells). Exhibits anti-proliferative activity and growth arrest in multiple cell lines (GI50 = 3.8, 0.79, and 6.3 µ,M in NIH 3T3, HeLa S3 and A549 cells, respectively). Shown to induce apoptotic cell death in liver cancer cell lines over-expressing LSF without affecting primary or immortalized hepatocytes. Also shown to inhibit hepatocellular carcinoma s.c. growth in mouse xenograft model without any toxic effects (1 mg/kg, i.p., once every 3 days).

Structure formula

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

Contents

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