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Fig. 2 Coumestrol is an ATP-competitive DYRK1A inhibitor. An enzyme-based assay was used to (A) evaluate the inhibitory effect of coumestrol on DYRK1A. (B) Assessment of the effect of ATP concentration on coumestrol's inhibition of DYRK1A activity. The inhibition of DYRK1A by coumestrol was determined to be an ATP-competitive inhibition with an IC50 value of 2.3 ?M.
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Reprinted from International journal of biological macromolecules, 282(Pt 4), Peng, C.H., Hwang, T.L., Hung, S.C., Tu, H.J., Tseng, Y.T., Lin, T.E., Lee, C.C., Tseng, Y.C., Ko, C.Y., Yen, S.C., Hsu, K.C., Pan, S.L., HuangFu, W.C., Identification, biological evaluation, and crystallographic analysis of coumestrol as a novel dual-specificity tyrosine-phosphorylation-regulated kinase 1A inhibitor, 136860, Copyright (2024) with permission from Elsevier. Full text @ Int. J. Biol. Macromol.