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TC-S 7005 is an inhibitor of polo-like kinase 2 (Plk2; IC50 = 4 nM).1 It is selective for Plk2 over Plk1 and Plk3 in a cell-free assay (IC50s = 214 and 24 nM, respectively). It induces mitotic arrest and cell death in HCT116 colorectal cancer cells. TC-S 7005 reduces IL-1β, IL-6, inducible nitric-oxide synthase (iNOS), and COX-2 levels in LPS-stimulated BV-2 microglial cells when used at a concentration of 8 µM and decreases NF-κB transcriptional activation in the same cells.2
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1. Design and synthesis of 2-
2. Polo-