AZ191 is a potent and selective DYRK1B inhibitor with IC50 of 17 nM in a cell-free assay, about 5- and 110-fold selectivity over DYRK1A and DYRK2, respectively.
(E) BEL7402 and HepG2 cells were treated with vehicle or 10 μM of the DYRK1B inhibitor, AZ191, alone and in combination with BafA1 for 24 h. Cyclin D1 expression was examined by immunoblot analysis.
ID-8 is a DYRK inhibitor, and sustains embryonic stem cell self-renewal in long-term culture.
Harmine, a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. It can also inhibit monoamine oxidases (MAOs) and cdc-like kinases (CLKs).