EHT 5372

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].

Product Specifications

CAS Number

[1425945-63-6]

UNSPSC

12352005

Target

CDK; DYRK; GSK-3

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Cancer; Metabolic Disease; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/eht-5372.html

Purity

98.12

Solubility

DMSO : 6.25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

N=C(C(S1)=NC2=C1C3=C(NC4=CC=C(Cl)C=C4Cl)N=CN=C3C=C2)OC

Molecular Formula

C17H11Cl2N5OS

Molecular Weight

404.27

References & Citations

[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.