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EHT 5372 是一种有效的、选择性的DYRK's 家族激酶抑制剂。EHT 5372抑制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。
EHT 5372 是一种有效的、选择性的DYRK's 家族激酶抑制剂。EHT 5372抑制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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 13,600 | 8-10周 | |
50 mg | ¥ 21,100 | 8-10周 |
产品描述 | EHT 5372 is a potent and selective inhibitor of DYRK’s family kinases. EHT 5372 shows IC 50 s 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. |
体外活性 | 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 [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 IC 50 of 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. |
分子量 | 404.27 |
分子式 | C17H11Cl2N5OS |
CAS No. | 1425945-63-6 |
存储 | Shipping with blue ice. |
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