EHT 5372

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 , respectively In Vitro EHT 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:Solid IC50& 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|)

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