Description
EHT 5372 is a highly potent and selective inhibitor of DYRK's family kinases with IC 50 s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, and 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, and GSK-3β, respectivelyIn VitroEHT 5372 (0.1-10 µM; 24 hours) dose-dependently reduces pS396-Tau levels with an IC 50 of 1.7 µM whereas cell viability remains over 87% in all conditions. EHT 5372 (0.01-1 µM) inhibits the direct phosphorylation of Tau by DYRK1AEHT 5372 reduces Aβ production in a dose-dependent reduction with an IC 50 of 1.06 µM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: HEK293 cells Concentration: 0.1, 0.5, 1, 5, 10 µM Incubation Time: 24 hours Result: Cell viability remained over 87% in all conditions. Western Blot AnalysisCell Line: HEK293 cells Concentration: 0.01, 0.03, 0.1, 0.3, 1 µM Incubation Time: Result: Potently and dose-dependently inhibited Tau phosphorylation at pS396.Form:SolidIC50& Target:DYRK1A:0.22 nM (IC:50:):DYRK1B:0.28 nM (IC:50:):DYRK2:10.8 nM (IC:50:):DYRK4:93.2 nM (IC:50:):CLK1:22.8 nM (IC:50:):CLK2:88.8 nM (IC:50:):CLK4:59.0 nM (IC:50:):GSK-3α:7.44 nM (IC:50:):GSK-3β:221 nM (IC:50:)