Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one, a Promising Inhibitor of DYRK1A

C Fruit, F Couly, R Bhansali, M Rammohan… - Pharmaceuticals, 2019 - mdpi.com
C Fruit, F Couly, R Bhansali, M Rammohan, MF Lindberg, JD Crispino, L Meijer, T Besson
Pharmaceuticals, 2019mdpi.com
Dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) hyperactivity has been
linked to the development of a number of human malignancies. DYRK1A is the most studied
family member, and the discovery of novel specific inhibitors is attracting considerable
interest. The 8-cyclopropyl-2 (pyridin-3-yl) thiazolo [5, 4-f] quinazolin-9 (8 H)-one (also called
FC162) was found to be a promising inhibitor of DYRK1A and was characterized in
biological experiments, by western transfer and flow cytometry on SH-SY5Y and pre-B cells …
Dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) hyperactivity has been linked to the development of a number of human malignancies. DYRK1A is the most studied family member, and the discovery of novel specific inhibitors is attracting considerable interest. The 8-cyclopropyl-2(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one (also called FC162) was found to be a promising inhibitor of DYRK1A and was characterized in biological experiments, by western transfer and flow cytometry on SH-SY5Y and pre-B cells. Here, the results obtained with FC162 are compared to well-characterized known DYRK1A inhibitors (e.g., Leucettine L41 and EHT1610).
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