EHT1610

EHT1610 (also known as EHT-1610) is a highly potent, selective, small-molecule inhibitor of dual-specificity tyrosine-phosphorylation-regulated kinases (DYRK), specifically targeting DYRK1A and DYRK1B with subnanomolar IC50 values (0.36 nM and 0.59 nM, respectively). Originally developed by ExonHit Therapeutics (later Diaxonhit, now Eurobio Scientific), EHT1610 has been widely utilized as a pharmacological probe to investigate the role of DYRK kinases in various disease models. In oncology, particularly in acute lymphoblastic leukemia (ALL) and Down syndrome-associated ALL (DS-ALL), EHT1610 has demonstrated significant antileukemic activity by regulating cell cycle progression, inducing apoptosis, and modulating key downstream signaling pathways such as FOXO1, STAT3, and cyclin D3. Additionally, EHT1610 has been studied in the context of neurodegenerative diseases like Alzheimer's disease and metabolic disorders such as type 1 diabetes.

Other names

methyl 9-((2-fluoro-4-methoxyphenyl)amino)thiazolo[5,4-f]quinazoline-2-carbimidate