EHT 5372 是一种高效选择性的DYRK's家族激酶抑制剂，对DYRK1A,DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, GSK-3β 的IC50分别为 0.22，0.28，10.8，93.2，22.8，88.8，59.0，7.44 和 221 nM。
| 生物活性 | EHT 5372 is a highly potent and selective inhibitor ofDYRK’sfamily kinases withIC50s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, 221 nM forDYRK1A,DYRK1B,DYRK2， DYRK3， CLK1, CLK2, CLK4,GSK-3α,GSK-3β[1][2]. |
| IC50& Target[1][2] | DYRK1A 0.22 nM (IC50) | DYRK1B 0.28 nM (IC50) | DYRK2 10.8 nM (IC50) | DYRK4 93.2 nM (IC50) | CLK1 22.8 nM (IC50) | CLK2 88.8 nM (IC50) | CLK4 59.0 nM (IC50) | GSK-3α 7.44 nM (IC50) | GSK-3β 221 nM (IC50) |
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体外研究
(In Vitro) | EHT 5372 (0.1-10 μM; 24 hours) dose-dependently reduces pS396-Tau levels with an IC50of 1.7 μM whereas cell viability remains over 87% in all conditions[1].
EHT 5372 (0.01-1 μM) inhibits the direct phosphorylation of Tau by DYRK1A[1]
EHT 5372 reduces Aβ production in a dose-dependent reduction with an IC50of 1.06 μM[1].
Cell Viability Assay[1] | 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[1] | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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