EHT 5372_product_DataBase

Bioactivity

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, and 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, and GSK-3β, respectively[1][2].

Invitro

EHT 5372 (0.1-10 μM; 24 hours) 剂量依赖性地降低 pS396-Tau 水平，IC50 值为 1.7 μM，而细胞活力在所有条件下均保持在 87% 以上[1]。EHT 5372 (0.01-1 μM) 通过对 DYRK1A 的抑制降低 Tau 蛋白的磷酸化水平[1]。EHT 5372 以剂量依赖性方式减少 Aβ 的产生，IC50 值为 1.06 μM[1]。 Cell Viability Assay[1] Cell Line:

Name

EHT 5372

CAS

1425945-63-6

Formula

C17H11Cl2N5OS

Molar Mass

404.27

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

EHT 5372

CAS: 1425945-63-6 F: C17H11Cl2N5OS W: 404.27