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Leucettinib-92

Catalog No. T79562   CAS 2732859-57-1

Leucettinib-92 (compound 92) is a kinase inhibitor selective for DYRK/CLK families, displaying IC50 values of 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), 1.0 μM (DYRK3), 0.52 μM (DYRK4), and 2.78 μM (GSK3) [1].

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Leucettinib-92 Chemical Structure
Leucettinib-92, CAS 2732859-57-1
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Leucettinib-92 (compound 92) is a kinase inhibitor selective for DYRK/CLK families, displaying IC50 values of 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), 1.0 μM (DYRK3), 0.52 μM (DYRK4), and 2.78 μM (GSK3) [1].
In vitro Leucettinib-92 (0.1-10 μM; 3 min) binds to DYRK1A in SH-SY5Y cells, stabilizing it to withstand melting temperatures above 52°C. Additionally, at a concentration of 1 μM, Leucettinib-92 inhibits the phosphorylation of two DYRK1A substrates, Thr212-Tau and Thr286-cyclin D1 [1].
Molecular Weight 378.49
Formula C21H22N4OS
CAS No. 2732859-57-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

Leucettinib-92 2732859-57-1 Cell Cycle/Checkpoint CDK inhibitor inhibit

 

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