EHT 5372 is a highly potent and selective inhibitor of DYRK’s family kinases with IC50s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, 221 nM for DYRK1A, DYRK1B , DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, GSK-3β.
体外研究
EHT 5372 (0.1-10 μM; 24 hours) dose-dependently reduces pS396-Tau levels with an IC50 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 DYRK1A
EHT 5372 reduces Aβ production in a dose-dependent reduction with an IC50 of 1.06 μM.
Cell Viability Assay
Cell 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 Analysis
Cell 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.
分子式
C17H11Cl2N5Os
分子量
404.27
CAS号
1425945-63-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.