Leucettine L41

Leucettine L41 is an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), DYRK2, CDC-like kinase 1 (CLK1), and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 µM, respectively). It also inhibits GSK3alpha/beta and Pim1 with IC50 values of 0.41 and 4.1 µM, respectively. It inhibits phosphorylation of the serine/arginine (SR) protein 9G8 by DYRK2, DYRK3, CLK1, CLK2, and CLK4 and inhibits TNF-alpha-induced SRp75 and SRp55 phosphorylation in human microvascular endothelial cells when used at concentrations ranging from 0.1 to 10 µM. Leucettine L41 modulates alternative pre-RNA splicing of a synthetic CLK1 minigene in a reporter model. It prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by amyloid-beta 25-35 (Cay-24155) in the hippocampus in a mouse model of Alzheimer's disease-like toxicity. Leucettine L41 (0.4, 1.2, and 4 µg, i.c.v.) also prevents memory deficits induced by amyloid-beta 25-35 in the same model.Formal Name: (5Z)-5-(1,3-benzodioxol-5-ylmethylene)-3,5-dihydro-2-(phenylamino)-4H-imidazol-4-one. CAS Number: 1112978-84-3. Molecular Formula: C17H13N3O3. Formula Weight: 307.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble, Ethanol: soluble. SMILES: O=C1N=C(NC2=CC=CC=C2)N/C1=C\C3=CC=C4C(OCO4)=C3. InChi Code: InChI=1S/C17H13N3O3/c21-16-13(8-11-6-7-14-15(9-11)23-10-22-14)19-17(20-16)18-12-4-2-1-3-5-12/h1-9H,10H2,(H2,18,19,20,21)/b13-8-. InChi Key: PGPHHJBZEGSUNE-JYRVWZFOSA-N.