Leucettine L41

CHF 70.00
In stock
AG-MR-C0023-M0011 mgCHF 70.00
AG-MR-C0023-M0055 mgCHF 280.00
AG-MR-C0023-M02525 mgCHF 980.00
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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
  • 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
  1. 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)
  2. 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)
  3. 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)
  4. Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines: G. Burgy, et al.; Eur. J. Med. Chem. 62, 728 (2013)
  5. 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)
  6. 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)
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