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LQZ-7I is an inhibitor of survivin.1 It inhibits survivin dimerization in a secreted alkaline phosphatase (SEAP) assay using DU145 prostate cancer cells expressing survivin and induces survivin degradation in C4-2 and PC3 prostate cancer cells in a proteasome-dependent manner. LQZ-7I is cytotoxic to C4-2 and PC3 cells (IC50s = 3.1 and 4.8 µM, respectively). It reduces tumor growth in a PC3 mouse xenograft model when administered at a dose of 100 mg/kg.
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1. Synthesis and identification of a novel lead targeting survivin dimerization for proteasome-