WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H562108
CAS#: 112978-84-3
Description: Leucettine L41 is a potent dual inhibitor of cdc2-like kinase (CLKs) and DYRKs.
Hodoodo Cat#: H562108
Name: Leucettine L41
CAS#: 112978-84-3
Chemical Formula: C17H13N3O3
Exact Mass: 307.10
Molecular Weight: 307.300
Elemental Analysis: C, 66.44; H, 4.26; N, 13.67; O, 15.62
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Synonym: Leucettine L41; Leucettine-L41; LeucettineL41; Leucettin L41;
IUPAC/Chemical Name: (5Z)-5-(1,3-Benzodioxol-5-ylmethylene)-3,5-dihydro-2-(phenylamino)-4H-imidazol-4-one
InChi Key: PGPHHJBZEGSUNE-JYRVWZFOSA-N
InChi Code: InChI=1S/C17H13N3O3/c21-16-13(8-11-6-7-14-15(9-11)23-10-22-14)19-17(20-16)18-12-4-2-1-3-5-12/h1-9H,10H2,(H2,18,19,20,21)/b13-8-
SMILES Code: O=C1NC(NC2=CC=CC=C2)=N/C1=C\C3=CC=C(OCO4)C4=C3
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
Soluble in DMSO | 0.0 | 100.00 |
The following data is based on the product molecular weight 307.30 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Naert G, Ferré V, Meunier J, Keller E, Malmström S, Givalois L, Carreaux F, Bazureau JP, Maurice T. 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. doi: 10.1016/j.euroneuro.2015.03.018. Epub 2015 Apr 10. PubMed PMID: 26381812.
2: Foucourt A, Hédou D, Dubouilh-Benard C, Girard A, Taverne T, Casagrande AS, Désiré L, Leblond B, Besson T. Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II. Molecules. 2014 Sep 26;19(10):15411-39. doi: 10.3390/molecules191015411. PubMed PMID: 25264830.
3: Fant X, Durieu E, Chicanne G, Payrastre B, Sbrissa D, Shisheva A, Limanton E, Carreaux F, Bazureau JP, Meijer L. cdc-like/dual-specificity tyrosine phosphorylation-regulated kinases inhibitor leucettine L41 induces mTOR-dependent autophagy: implication for Alzheimer's disease. Mol Pharmacol. 2014 Mar;85(3):441-50. doi: 10.1124/mol.113.090837. Epub 2013 Dec 23. PubMed PMID: 24366666.
4: Burgy G, Tahtouh T, Durieu E, Foll-Josselin B, Limanton E, Meijer L, Carreaux F, Bazureau JP. Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. Eur J Med Chem. 2013 Apr;62:728-37. doi: 10.1016/j.ejmech.2013.01.035. Epub 2013 Feb 6. PubMed PMID: 23454515.
5: Tahtouh T, Elkins JM, Filippakopoulos P, Soundararajan M, Burgy G, Durieu E, Cochet C, Schmid RS, Lo DC, Delhommel F, Oberholzer AE, Pearl LH, Carreaux F, Bazureau JP, Knapp S, Meijer L. Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. J Med Chem. 2012 Nov 8;55(21):9312-30. doi: 10.1021/jm301034u. Epub 2012 Oct 8. PubMed PMID: 22998443.
6: Debdab M, Carreaux F, Renault S, Soundararajan M, Fedorov O, Filippakopoulos P, Lozach O, Babault L, Tahtouh T, Baratte B, Ogawa Y, Hagiwara M, Eisenreich A, Rauch U, Knapp S, Meijer L, Bazureau JP. 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. doi: 10.1021/jm200274d. Epub 2011 May 26. PubMed PMID: 21615147.