AZ Dyrk1B 33 是\u200b\u200b一种有效的选择性 Dyrk1B 激酶抑制剂,IC50 为 7 nM。
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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 activity (IC50 = 194 nM). Exhibits better selectivity than AZ 191 ; displays no off-target effects against a panel of 124 kinases tested (no kinase was inhibited above 50% at 1 μM).
Kettle et al (2015) Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis. J.Med.Chem. 58 2834 PMID:25738750
MEK162 (ARRY-162, ARRY-438162)
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