DYRK2-IN-2 (Compound C17) is a selective inhibitor of DYRK2, with its IC50 value being 40.3 nM. The inhibitory activity of DYRK2-IN-2 on DYRK1A ( IC50 = 1842 nM), DYRK1B ( IC50 = 1335 nM), DYRK4 ( IC50 = 1931 nM), DYRK3 ( IC50 = 112 nM), and CLKs ( IC50 = 540-6496 NM) is relatively low. DYRK2-IN-2 inhibits the phosphorylation of Tau protein at Thr212 and shows moderate cytotoxicity in HT22 cells. DYRK2-IN-2 can be used in cancer research [1].
References:
[1]. Lindberg MF, et al. Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases. J Med Chem. 2023 Mar 23;66(6):4106-4130.
References:
[1]. Lindberg MF, et al. Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases. J Med Chem. 2023 Mar 23;66(6):4106-4130.