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 ?M, respectively). It reduces tumor growth in a PC3 mouse xenograft model when administered at a dose of 100 mg/kg.
1.Peery, R., Kyei-Baffour, K., Dong, Z., et al.Synthesis and identification of a novel lead targeting survivin dimerization for proteasome-dependent degradationJ. Med. Chem.63(13)7243-7251(2020)