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AdipoGen Life Sciences
Leucettine L41
70
CHF
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
| 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 |
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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