EHT 5372

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

EHT 5372 

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。

EHT 5372

EHT 5372 Chemical Structure

CAS No. : 1425945-63-6

规格 价格 是否有货
5 mg ￥4500 询问价格 & 货期
10 mg ￥8000 询问价格 & 货期
25 mg ￥16500 询问价格 & 货期
50 mg ￥25500 询问价格 & 货期
100 mg ￥38000 询问价格 & 货期

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生物活性

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[1][2].

IC50 & Target[1][2]

DYRK1A

0.22 nM (IC50)

DYRK1B

0.28 nM (IC50)

DYRK2

10.8 nM (IC50)

DYRK3

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)

体外研究
(In Vitro)

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[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 IC50 of 1.06 μM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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

Formula

C17H11Cl2N5OS
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.
参考文献

  • [1]. Séverine Coutadeur, et al. A novel DYRK1A (dual specificity tyrosine phosphorylation-regulated kinase 1A) inhibitor for the treatment of Alzheimer’s disease: effect on Tau and amyloid pathologies in vitro. J Neurochem. 2015 May;133(3):440-51.

    [2]. Apirat Chaikuad, et al. An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases. J Med Chem. 2016 Nov 23;59(22):10315-10321.

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