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EHT 5372

CAS No. : 1425945-60-3

MCE 站：EHT 5372

产品活性：EHT 5372 是双特异性酪氨酸磷酸化调节酶 (DYRK) 的强效抑制剂，其 IC₅₀ 值分别为 0.22，0.28 nM。

研究领域：Protein Tyrosine Kinase/RTK  |  Cell Cycle/DNA Damage  |  PI3K/Akt/mTOR  |  Stem Cell/Wnt

作用靶点：DYRK  |  CDK  |  GSK-3

In Vitro: EHT 5372 is a strong inhibitor of DYRK’s family kinases, with IC₅₀s of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively. IC₅₀ 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 glycogen synthase kinase 3 (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.

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