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Poloxin is an inhibitor of the polo-like kinase 1 (Plk1) polo-box domain (PBD; apparent IC50 = 4.8 µM).1 It is selective for the Plk1 PBD over Plk2 and Plk3 PBDs (IC50s = 18.7 and 53.9 µM, respectively). Poloxin (5, 10, and 25 µM) induces cell cycle arrest at the G2/M phase, apoptosis, and mislocalization of Plk1 in HeLa cells. It reduces cell proliferation in a panel of 10 cancer cell lines (EC50s = 15-35 µM).2 In vivo, poloxin (40 mg/kg) reduces tumor growth and induces intratumor apoptosis in an MDA-MB-231 breast cancer mouse xenograft model.
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1. Inhibition of polo-
2. Polo-