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Leucettinib-92 (compound 92) is a kinase inhibitor selective for the DYRK/CLK families, 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 [1].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | Inquiry | 8-10 weeks | |
50 mg | Inquiry | 8-10 weeks |
Description | Leucettinib-92 (compound 92) is a kinase inhibitor selective for the DYRK/CLK families, 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 [1]. |
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]. |
Molecular Weight | 378.49 |
Formula | C21H22N4OS |
Cas No. | 2732859-57-1 |
Storage | Shipping with blue ice. |
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