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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 should be used as a negative control together with this compound.
Product References
Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases: M.F. Lindberg, et al.; J. Med. Chem. 66, 4106 (2023)
Leucettinibs, a Class of DYRK/CLK Kinase Inhibitors Inspired by the Marine Sponge Natural Product Leucettamine B: E. Deau, et al.; J. Med. Chem. 66, 10694 (2023)