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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 | - | In Stock |
| 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 | CLK3:0.8 μM, DYRK1A:124 nM, CLK1:147 nM, DYRK3:1.0 μM, DYRK2:0.16 μM, CLK4:5.2 nM, CLK2:39 nM, GSK3:2.78 μM, DYRK1B:204 nM, DYRK4:0.52 μM |
| 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 |
| Color | Yellow |
| Appearance | Solid |
| 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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DMSO
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