Leucettine L41

Names

[ Name ]:
Leucettine L41

[Synonym ]:
(5Z)-2-Anilino-5-(1,3-benzodioxol-5-ylmethylene)-1,5-dihydro-4H-imidazol-4-one
leucettine L41
4H-Imidazol-4-one, 5-(1,3-benzodioxol-5-ylmethylene)-3,5-dihydro-2-(phenylamino)-, (5Z)-

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> DYRK

Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

Research Areas >> Neurological Disease

[References]

[1]. Debdab M, 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. 2011 Jun 23;54(12):4172-86.

[2]. Naert G, 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. 2015 Nov;25(11):2170-82.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C₁₇H₁₃N₃O₃

[ Molecular Weight ]:
307.303

[ Exact Mass ]:
307.095703

[ LogP ]:
3.49

[ Index of Refraction ]:
1.698

Related Compounds

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