AdipoGen Life Sciences

Leucettine L41

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AG-MR-C0023-M0011 mgCHF 70.00

AG-MR-C0023-M0055 mgCHF 280.00

AG-MR-C0023-M02525 mgCHF 980.00

Specifications / Handling

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Product Details
Synonyms	(5Z)-5-(1,3-Benzodioxol-5-yl)methylene-2-phenylamino-3,5-dihydro-4H-imidazol-4one
Product Type	Chemical
Properties
Formula	C₁₇H₁₃N₃O₃
MW	307.3
CAS	1112978-84-3
Purity Chemicals	≥98% (NMR)
Appearance	Beige solid.
Solubility	Soluble in DMSO or ethanol.
Reconstitution	Stock solutions can be made up to 10mM in DMSO.
Identity	Determined by ¹H-NMR.
InChi Key	PGPHHJBZEGSUNE-JYRVWZFOSA-N
Smiles	O=C1NC(NC2=CC=CC=C2)=N\C1=C/C1=CC2=C(OCO2)C=C1
Shipping and Handling
Shipping	AMBIENT
Short Term Storage	+4°C
Long Term Storage	-20°C
Handling Advice	Keep cool and dry. Protect from light and moisture.
Use/Stability	Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS	Download PDF
Product Specification Sheet
Datasheet	Download PDF

Product-specific References

Description

Potent inhibitor of DYRKs (DYRK1A (IC₅₀=40nM); DYRK2 (IC₅₀=35nM)) and CLKs (CLK1, CLK3). Interacts also with GSK-3α/β, CK2 and PIM1.
Interacts with the complex PIKfyve/Vac14/Fig4.
Modulates alternative splicing of pre-mRNA in various cellular systems.
Neuroprotective against APP-induced cell death.
Tools to study and modulate pre-RNA splicing. Potential compound for Alzheimer's disease and diseases involving abnormal pre-mRNA splicing.
Potential compound to study Down syndrome (inhibition of DYRK1A).
Neuroprotective against glutamate-induced cell death.
Autophagy activator.

Product References

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: M. Debdab, et al.; J. Med. Chem. 54, 4172 (2011)
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B: T. Tahtouh, et al.; J. Med. Chem. 55, 9312 (2012)
Leucettines, a family of pharmacological inhibitors of DYRKs & CLKs kinases derived from the marine sponge Leucettamine B: T. Tahtouh, et al.; Planta Med. 78, (2012)
Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines: G. Burgy, et al.; Eur. J. Med. Chem. 62, 728 (2013)
Cdc-like/dual-specificity tyrosine phosphorylation-regulated kinases inhibitor leucettine L41 induces mTOR-dependent autophagy: implication for Alzheimer's disease: X. Fant, et al.; Mol. Pharmacol. 85, 441 (2014)
Marine-Derived 2-Aminoimidazolone Alkaloids. Leucettamine B-Related Polyandrocarpamines Inhibit Mammalian and Protozoan DYRK & CLK Kinases: N. Loaec, et al.; Mar. Drugs 15, 316 (2017) (Review)
Chemically defined and growth-factor-free culture system for the expansion and derivation of human pluripotent stem cells: S. Yasuda, et al.; Nature Biomed. Eng. 2, 173 (2018)
Correction of cognitive deficits in mouse models of Down syndrome by a pharmacological inhibitor of DYRK1A: T.L. Nguyen, et al.; Dis. Model Mech. 11, dmm035634 (2018)
Combined Inhibition of DYRK1A, SMAD, and Trithorax Pathways Synergizes to Induce Robust Replication in Adult Human Beta Cells: P. Wang, et al.; Cell Metab. 29, 638 (2019)
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)
Chemical, Biochemical, Cellular, and Physiological Characterization of Leucettinib-21, a Down Syndrome and Alzheimer’s Disease Drug Candidate: M.F. Lindberg, et al.; J. Med. Chem. 66, 15648 (2023)

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