EHT-5372 is a potent and selective DYRK1A inhibitor (IC50 = 0.22 nM). EHT-5372 shows high degree of selectivity over 339 kinases. EHT 5372 inhibits DYRK1A-induced Tau phosphorylation at multiple AD-relevant sites in bioactive compound and cellular assays. EHT 5372 also normalizes both Aβ-induced Tau phosphorylation and DYRK1A-stimulated Aβ production. EHT 5372 inhibits DYRK1A-induced Tau phosphorylation, Aβ production and Aβ effects on phospho-Tau, including Tau aggregation. References: Chaikuad A, Diharce J, Schroder M, Foucourt A, Leblond B, Casagrande AS, Desire L, Bonnet P, Knapp S, Besson T. 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 Oct 21. [Epub ahead of print] PubMed PMID: 27766861.

纯度：≥98%

CAS：1425945-63-6