EHT 5372 is a strong DYRK’s family kinases of inhibitor (IC50s: 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively).

IC50s for DYRK2 and DYRK3 were higher (10.8 and 93.2 nM, respectively) and there was no inhibition on DYRK4. EHT 5372 displayed minimal impact on the CDC2-like kinase (CLK) family, with more than 100x selectivity over CLK1 (CLK1: IC50=22.8 nM; CLK2: IC50=88.8 nM; CLK3: IC50>10 lM; CLK4: no inhibition) and on the GSK3 family (GSK3α: IC50=7.44 nM; GSK3β: IC50=221 nM). EHT 5372 inhibits the direct phosphorylation of Tau by DYRK1A. EHT 5372 also normalizes both Aβ-induced Tau phosphorylation and DYRK1A-stimulated Aβ production [2].

1425945-60-3

C18H14FN5O2S

383.4

EHT 5372;EHT 1610

DMSO:25 mg/mL (65.21 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years