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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

Leucettinib-92

😃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 SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$768-10 weeks8-10 weeks
5 mg$185-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
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].
SynonymsLeucettinib-92, Leucettinib92, Leucettinib 92
Chemical Properties
Molecular Weight378.49
FormulaC21H22N4OS
Cas No.2732859-57-1
SmilesN(C12CC3CC(C1)CC(C2)C3)C=4N/C(=C\C=5C=C6C(=CC5)N=CS6)/C(=O)N4
ColorYellow
AppearanceSolid
Storage & Solubility Information
Storagestore 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.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6421 mL13.2104 mL26.4208 mL132.1039 mL
5 mM0.5284 mL2.6421 mL5.2842 mL26.4208 mL
10 mM0.2642 mL1.3210 mL2.6421 mL13.2104 mL
20 mM0.1321 mL0.6605 mL1.3210 mL6.6052 mL
50 mM0.0528 mL0.2642 mL0.5284 mL2.6421 mL

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