| Bioactivity | Leucettinib-92 (compound 92) is an inhibitor of DYRK/CLK kinase, The IC50s are 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), respectively. 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3)[1]. |
| Target | IC50: 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), 2.78 μM (GSK3) |
| Invitro | Leucettinib-92 (0.1-10 μM; 3 min) 与 SH-SY5Y 细胞中的 DYRK1A 结合，诱导其稳定直到 52°C 以上的熔化温度。Leucettinib-92 (1 μM) 抑制 2 种 DYRK1A 底物 (Thr212-Tau and Thr286-cyclin D1) 的磷酸化[1]。 0 --> Leucettinib-92 相关抗体: |
| Name | Leucettinib-92 |
| CAS | 2732859-57-1 |
| Formula | C21H22N4OS |
| Molar Mass | 378.49 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Deau E, et al. Leucettinibs, a Class of DYRK/CLK Kinase Inhibitors Inspired by the Marine Sponge Natural Product Leucettamine B. J Med Chem. 2023 Aug 10;66(15):10694-10714. |
Leucettinib-92
CAS: 2732859-57-1 F: C21H22N4OS W: 378.49
Leucettinib-92 (compound 92) is an inhibitor of DYRK/CLK kinase, The IC50s are 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4
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