Leucettine L41
Based on 1 publication(s) in Google Scholar
Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) and CDC-like kinases (CLKs). Leucettine L41 can also inhibit GSK-3 singnaling. Leucettine L41 can inhibit cell apoptosis and ROS production. Leucettine L41 can promote β-cell cell cycle progression, cell proliferation and increase insulin secretion. Leucettine L41 can be used for the researches of neurological disease and metabolic disease, such as Alzheimer’s disease (AD) and diabetes.
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- Pureza: 98.98%
- No. CAS: 1112978-84-3
- Fòrmula: C17H13N3O3
- Peso molecular:307.30
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Leucettine L41
More
Actividad biológica
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DYRK1A 10-60 nM (IC50) |
DYRK1B 44 nM (IC50) |
CLK4 64 nM (IC50) |
CLK1 71 nM (IC50) |
DYRK2 73 nM (IC50) |
GSK-3α/β 210-410 nM (IC50) |
DYRK3 320 nM (IC50) |
DYRK4 520 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HT-22 | EC50 |
6.02 μM
Compound: L41
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Neuroprotective activity against glutamate-induced cell death in mouse HT-22 cells treated for 24 hrs by MTS assay
Neuroprotective activity against glutamate-induced cell death in mouse HT-22 cells treated for 24 hrs by MTS assay
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[PMID: 34928152] |
| HT-22 | IC50 |
>100 μM
Compound: 20
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Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
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[PMID: 36876904] |
| HT-22 | IC50 |
>20 μM
Compound: L41
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Neurotoxicity against mouse HT-22 cells assessed as cell survival treated for 24 hrs by MTS assay
Neurotoxicity against mouse HT-22 cells assessed as cell survival treated for 24 hrs by MTS assay
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[PMID: 34928152] |
Leucettine L41 (0.01-100 μM) increases viability and proliferation in MIN6 cells[2].
Leucettine L41 (5 μM, 24 h) increases cells in G2/M phase in MIN6 cells[2].
Leucettine L41 (5 μM, 24 h) increases insulin and C-peptide production in MIN6 cells[2].
Leucettine L41 improves insulin secretion in isolated mouse islets[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MIN6 cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Showed cells in phase G2/M reaching almost 45%.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Aβ25-35-treated mice[1]
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Dosage:0.4, 1.2 and 4 μg
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Administration:Intracerebrally injection
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Result:Reduced lipid peroxidation levels and ROS accumulation.
Decreased AKT activation and increased GSK-3β activation.
Decreased Tau phosphorylation.
Increased Bcl-2 levels and decreased Bax levels in hippocampus.
Chemical Information
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No. CAS 1112978-84-3
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Appearance Solid
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Peso molecular 307.30
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Fòrmula C17H13N3O3
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Color Light yellow to yellow
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SMILES
O=C1NC(NC2=CC=CC=C2)=N/C1=C\C3=CC=C(OCO4)C4=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : 100 mg/mL (325.41 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (8.14 mM); Clear solution; Need ultrasonic and warming and heat to 80°C
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. 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. [Content Brief]
[2]. Pucelik B, et al. DYRK1A inhibitors leucettines and TGF-β inhibitor additively stimulate insulin production in beta cells, organoids, and isolated mouse islets. PLoS One. 2023 May 17;18(5):e0285208. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2541 mL | 16.2707 mL | 32.5415 mL | 81.3537 mL |
| 5 mM | 0.6508 mL | 3.2541 mL | 6.5083 mL | 16.2707 mL | |
| 10 mM | 0.3254 mL | 1.6271 mL | 3.2541 mL | 8.1354 mL | |
| 15 mM | 0.2169 mL | 1.0847 mL | 2.1694 mL | 5.4236 mL | |
| 20 mM | 0.1627 mL | 0.8135 mL | 1.6271 mL | 4.0677 mL | |
| 25 mM | 0.1302 mL | 0.6508 mL | 1.3017 mL | 3.2541 mL | |
| 30 mM | 0.1085 mL | 0.5424 mL | 1.0847 mL | 2.7118 mL | |
| 40 mM | 0.0814 mL | 0.4068 mL | 0.8135 mL | 2.0338 mL | |
| 50 mM | 0.0651 mL | 0.3254 mL | 0.6508 mL | 1.6271 mL | |
| 60 mM | 0.0542 mL | 0.2712 mL | 0.5424 mL | 1.3559 mL | |
| 80 mM | 0.0407 mL | 0.2034 mL | 0.4068 mL | 1.0169 mL | |
| 100 mM | 0.0325 mL | 0.1627 mL | 0.3254 mL | 0.8135 mL |
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