ARN25699 is a kinase inhibitor with an IC50 of 5.5 nM against GSK-3β, 2.2 nM against FYN-α, and 242.3 nM against DYRK1A, and it exhibits oral bioavailability. ARN25699 reduces hyperphosphorylation of tau protein and promotes microtubule bundle formation. ARN25699 has a broader kinome inhibitory profile and targets kinases associated with the pathogenic mechanisms linked to Alzheimer's disease. ARN25699 can be used in the research of Alzheimer's disease and related tauopathies [1].
In Vitro, ARN25699 (Compound 28) (0.1-10 μM) inhibits a subset of kinases associated with the pathogenesis of Alzheimer's disease[1]. ARN25699 (1-100 μM; 6 h) induces dose-dependent microtubule bundle formation in Tau0N4R-TM-tGFP U2OS cells[1].
References:
[1]. Demuro S, et al. A Polypharmacology-Driven Approach to Alzheimer's Disease and Tauopathies: Rational Design, Synthesis and Characterization of Amino-Pyrazole-Based Multikinase (GSK-3β/FYN-α/DYRK1A) Inhibitors. J Med Chem. 2026 May 14;69(9):9991-10018.
In Vitro, ARN25699 (Compound 28) (0.1-10 μM) inhibits a subset of kinases associated with the pathogenesis of Alzheimer's disease[1]. ARN25699 (1-100 μM; 6 h) induces dose-dependent microtubule bundle formation in Tau0N4R-TM-tGFP U2OS cells[1].
References:
[1]. Demuro S, et al. A Polypharmacology-Driven Approach to Alzheimer's Disease and Tauopathies: Rational Design, Synthesis and Characterization of Amino-Pyrazole-Based Multikinase (GSK-3β/FYN-α/DYRK1A) Inhibitors. J Med Chem. 2026 May 14;69(9):9991-10018.