Inhibitor of cdc2-like kinases (Clk) and DYRK kinases (IC50
values are 68, 68 and 231 nM for Clk1, Clk4 and Clk2, respectively, and 282 and 1156 nM for Dyrk1A and Dyrk1B). Shows 20-fold selectivity for Clk4 over Dyrk1A. Stable in both mouse and human plasma. Moderately cell permeable.
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Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315.
Coombs et al.