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Beschreibung

A cell-permeable vanillin-derived pyridyl-ethanamine compound that acts as a highly potent type II Plk1 inhibitor (IC50 of 200 pM) and targets the less conserved DFG motif that is only accessible when the kinase is in its inactive DFG-out conformation, resulting in an excellent selectivity over Plk2 (IC50 >66 µ,M), Plk3 (IC50 = 875 nM), and aurora A kinase (no detectable effect). Shown to inhibit the proliferation of HeLa cells with an EC50 of 18 µ,M.