EHT-5372

• CAT Number: I006632
• CAS Number: 1425945-63-6
• Molecular Formula: C17H11Cl2N5OS
• Molecular Weight: 404.269
• Purity: ≥95%
• Target: DYRK1A inhibitor
• Solubility: Soluble in DMSO
• Storage: 0 - 4°C for short term or -20 °C for long term

EHT-5372 (Cat.No:I006632) 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 biochemical 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.

Reference

1:J Med Chem. 2016 Nov 23;59(22):10315-10321. Epub 2016 Nov 2. 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.Chaikuad A,Diharce J,Schröder M,Foucourt A,Leblond B,Casagrande AS,Désiré L,Bonnet P,Knapp S,Besson T, PMID: 27766861 DOI: 10.1021/acs.jmedchem.6b01083 Abstract: Methyl 9-anilinothiazolo[5,4-f]quinazoline-2-carbimidates 1 (EHT 5372) and 2 (EHT 1610) are strong inhibitors of DYRK/’s family kinases. The crystal structures of the complex revealed a noncanonical binding mode of compounds 1 and 2 in DYRK2, explaining the remarkable selectivity and potency of these inhibitors. The structural data and comparison presented here provide therefore a template for further improvement of this inhibitor class and for the development of novel inhibitors selectively targeting DYRK kinases.