DYRK2-IN-2 hydrochloride is a selective DYRK2 inhibitor with an IC50 of 40.3 nM. DYRK2-IN-2 hydrochloride shows weaker inhibitory activity against DYRK1A ( IC50 = 1842 nM), DYRK1B ( IC50 = 1335 nM), DYRK4 ( IC50 = 1931 nM), DYRK3 ( IC50 = 112 nM) and CLK ( IC50 = 540-6496 nM). DYRK2-IN-2 hydrochloride inhibits the phosphorylation of Thr212 in Tau protein. DYRK2-IN-2 hydrochloride is applicable for neuronal research [1].
In Vitro, DYRK2-IN-3 (Compound C17) (up to 10 μM) hydrochloride potently and selectively inhibits recombinant DYRK2 with an IC50 of 0.0403 μM; it shows weak activity against other kinases of the DYRK and CLK families, and no activity against CDK5/p25, CK1ε or GSK3β[1]. DYRK2-IN-3 (1-30 μM; 6 h) hydrochloride potently and dose-dependently inhibits Thr212-Tau phosphorylation in SH-SY5Y cells expressing 4R-Tau[1]. DYRK2-IN-3 (48 h) hydrochloride exhibits cytotoxicity against HT22 cells, with an IC50 of 14.7 μM following 48 h of exposure[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.
In Vitro, DYRK2-IN-3 (Compound C17) (up to 10 μM) hydrochloride potently and selectively inhibits recombinant DYRK2 with an IC50 of 0.0403 μM; it shows weak activity against other kinases of the DYRK and CLK families, and no activity against CDK5/p25, CK1ε or GSK3β[1]. DYRK2-IN-3 (1-30 μM; 6 h) hydrochloride potently and dose-dependently inhibits Thr212-Tau phosphorylation in SH-SY5Y cells expressing 4R-Tau[1]. DYRK2-IN-3 (48 h) hydrochloride exhibits cytotoxicity against HT22 cells, with an IC50 of 14.7 μM following 48 h of exposure[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.