| Identification | Back Directory | [Name]
Leucettine L41 | [CAS]
1112978-84-3 | [Synonyms]
Leucettine L41
Leucettine L41,Leucettine L-41
4H-Imidazol-4-one, 5-(1,3-benzodioxol-5-ylmethylene)-3,5-dihydro-2-(phenylamino)-, (5Z)- | [Molecular Formula]
C17H13N3O3 | [MOL File]
1112978-84-3.mol | [Molecular Weight]
307.3 |
| Hazard Information | Back Directory | [Description]
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).1 It also inhibits GSK3α/β 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-α-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-β 25-35 in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity.2 Leucettine L41 (0.4, 1.2, and 4 μg, i.c.v.) also prevents memory deficits induced by amyloid-β 25-35 in the same model. | [Uses]
Leucettine L41 is a potent 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)[1]. Leucettine L41 prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by Aβ25-35 in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity. Leucettine L41 also prevents memory deficits induced by Aβ25-35 in the same model[2]. | [References]
1. Debdab, M., Carreaux, F., Renault, S., et al. Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: Modulation of alternative pre-RNA splicing J. Med. Chem. 54(12),4172-4186(2011).
2. Naert, G., Ferré, V., Meunier, J., et al. Leucettine L41, a DYRK1A-preferential DYRKs/CLKs inhibitor, prevents memory impairments and neurotoxicity induced by oligomeric Aβ25-35 peptide administration in mice Eur. Neuropsychopharmacol. 25(11),2170-2182(2015). |
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| Company Name: |
InvivoChem
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| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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