Potent and selective ATP-competitive Dyrk1B kinase inhibitor (IC50
= 7 nM); displays distinct cellular effects when compared to DYRK1B knockdown through siRNA. Demonstrates cellular in vitro
= 194 nM). Exhibits better selectivity than AZ 191
(Cat. No 5232); displays no off-target effects against a panel of 124 kinases tested (no kinase was inhibited above 50% at 1 μ
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Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis.
Kettle et al.