Fig. 3: Discovery of the highly selective DYRK2 inhibitor YK-2-69. | Nature Communications

Fig. 3: Discovery of the highly selective DYRK2 inhibitor YK-2-69.

From: Targeting dual-specificity tyrosine phosphorylation-regulated kinase 2 with a highly selective inhibitor for the treatment of prostate cancer

Fig. 3: Discovery of the highly selective DYRK2 inhibitor YK-2-69.

a Flowchart of virtual screening to discover the hit DYRK2 inhibitor compound 12. b Chemical structure and activities of YK-2-69. c Inhibitory activity of YK-2-69 against DYRK1A, 1B, 2, 3, and 4. d Kinase selectivity experiment of YK-2-69 (1 µM) was carried out at Reaction Biology Corporation (https://www.reactionbiology.com/). The dot size indicates the inhibitory rate. A dot represents a type of kinase and the red dot represents DYRK2. e Validation of interaction of p-4E-BP1 (Thr37/46) with DYRK2 by co-immunoprecipitation assay. 1% volume of cell lysate was used as input. f Western blotting analysis of indicated proteins after treatment with DMSO or YK-2-69 for 48 h. The special bands of 4E-BP1 and p-4E-BP1 were shown with arrows. Source data are provided as a Source Data file.

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