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Leucettinib-92
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Catalog No. T79562Cas No. 2732859-57-1
Alias Leucettinib-92, Leucettinib92, Leucettinib 92
Leucettinib-92 is a small-molecule inhibitor of the DYRK and CLK kinase families that exhibits differential inhibitory activity across multiple kinases, with IC50 values of 147 nM for CLK1, 39 nM for CLK2, 5.2 nM for CLK4, 0.8 μM for CLK3, 124 nM for DYRK1A, 204 nM for DYRK1B, 0.16 μM for DYRK2, 1.0 μM for DYRK3, 0.52 μM for DYRK4, and 2.78 μM for GSK3, supporting its use in kinase signaling and regulatory mechanism research.
Leucettinib-92
Copy Product Info😃Good
Catalog No. T79562Alias Leucettinib-92, Leucettinib92, Leucettinib 92Cas No. 2732859-57-1
Leucettinib-92 is a small-molecule inhibitor of the DYRK and CLK kinase families that exhibits differential inhibitory activity across multiple kinases, with IC50 values of 147 nM for CLK1, 39 nM for CLK2, 5.2 nM for CLK4, 0.8 μM for CLK3, 124 nM for DYRK1A, 204 nM for DYRK1B, 0.16 μM for DYRK2, 1.0 μM for DYRK3, 0.52 μM for DYRK4, and 2.78 μM for GSK3, supporting its use in kinase signaling and regulatory mechanism research.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $76 | 8-10 weeks | 8-10 weeks | |
| 5 mg | $185 | 8-10 weeks | 8-10 weeks |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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| Description | Leucettinib-92 is a small-molecule inhibitor of the DYRK and CLK kinase families that exhibits differential inhibitory activity across multiple kinases, with IC50 values of 147 nM for CLK1, 39 nM for CLK2, 5.2 nM for CLK4, 0.8 μM for CLK3, 124 nM for DYRK1A, 204 nM for DYRK1B, 0.16 μM for DYRK2, 1.0 μM for DYRK3, 0.52 μM for DYRK4, and 2.78 μM for GSK3, supporting its use in kinase signaling and regulatory mechanism research. |
| Targets&IC50 | CLK1:147 nM, DYRK1B:204 nM, DYRK2:0.16 μM, GSK3:2.78 μM, DYRK4:0.52 μM, DYRK3:1.0 μM, CLK3:0.8 μM, CLK2:39 nM, DYRK1A:124 nM, CLK4:5.2 nM |
| In vitro | Leucettinib-92 (0.1-10 μM; 3 min) binds to DYRK1A in SH-SY5Y cells, stabilizing the enzyme to withstand melting temperatures above 52°C, and at 1 μM, it inhibits the phosphorylation of DYRK1A substrates Thr212-Tau and Thr286-cyclin D1 [1]. |
| In vivo | Method: Leucettinib-92 was administered in vivo to prediabetic and diabetic GK rats to assess β-cell proliferation, insulin secretion, glucose tolerance, and insulin sensitivity. Result: Leucettinib-92 increased β-cell proliferation and mass, prevented hyperglycemia development, reduced basal hyperglycemia, and improved glucose tolerance and insulin secretion[1]. |
| Synonyms | Leucettinib-92, Leucettinib92, Leucettinib 92 |
| Molecular Weight | 378.49 |
| Formula | C21H22N4OS |
| Cas No. | 2732859-57-1 |
| Smiles | N(C12CC3CC(C1)CC(C2)C3)C=4N/C(=C\C=5C=C6C(=CC5)N=CS6)/C(=O)N4 |
| Storage | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 20 mg/mL (52.84 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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