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Beschreibung

A cell-permeable thiazolamide compound that acts as a potent, reversible, and ATP-competitive inhibitor against casein kinase-2/CK2 (IC50 = 32 and 46 nM against CK2alpha and CK2alpha', respectively), as well as DYRK1B and FLt-3 (82% and 76% inhibition, respectively, at 30 nM), while diplaying reduced or little potency toward other targets in a 70-kinase panel selectivity profile study. Shown to effectively block the proliferation of a variety of cancer cells (IC50 = 2.6, 1.6, and 2.4 µ,M, in A549, HCT116, and MCF-7 cultures, respectively).