Leucettinib-92 is a potent DYRK/CLK inhibitor, inhibits CLK1, CLK2, CLK4, DYRK1A and DYRK1B with IC50 of 9.2, 6, 6, 1.2 and 1.8 nM, respectively.
Leucettinib-92 preferably targets CLK1, CLK2, CLK4, DYRK1A and DYRK1B on the Eurofins DiscovRx KinomeScan selectivity panel (468 kinases) at 1 uM.
Leucettinib-92 can penetrate cells and inhibits DYRK1A at low concentrations (from 0.1–0.3 μM) in cell models.
