Potent inhibitor of DYRK1A (IC50=1.2nM), DYRK1B (IC50=1.8nM), DYRK3 (IC50=19.3nM) and CLK2 (IC50=0.6nM) [1]. Inhibits the phosphorylation of Tau at Thr212 and cyclin D1 at Thr286. Corrects cognitive deficits in animal models of Down syndrome. iso-Leucettinib-92 (Prod. No. AG-MR-C0050) is a kinase-inactive isomer and...

Description: Leucettinib-92 (compound 92) is a kinase inhibitor selective for the DYRK/CLK families, with IC50 values of 147 nM for CLK1, 39 nM for CLK2, 5.2 nM for CLK4, 0.8 µM for CLK3, 124 nM for DYRK1A, 204 nM for DYRK1B, 0.16 µM for DYRK2, 1.0 µM for DYRK3, 0.52 µM for DYRK4, and 2.78 µM for GSK3 [1]. Target: CDK