Welcome to ProbeChem!Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : ZJCK-6-46
Catalog No.: PC-22747Not For Human Use, Lab Use Only.
ZJCK-6-46 is a potent, selective, and orally available dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor with IC50 of 0.68 nM.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
ZJCK-6-46 is a potent, selective, and orally available dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor with IC50 of 0.68 nM.
ZJCK-6-46 significantly inhibits the activity of DYRK1B (IC50=1.02 nM), shows weak activity against other three DYRK isoforms(DYRK2, IC50 = 14.18 nM; DYRK3, IC50 = 17.48 nM; DYRK4, IC50 = 401.3 nM).
ZJCK-6-46 also inhibits the activities of CLKs, especially, CLK1 and CLK4 (IC50 = 1.68 and 1.80 nM, respectively), while CLK3 shows relatively less sensitiveness (IC50 = 38.91 nM).
ZJCK-6-46 significantly decreases DYRK1A-mediated phosphorylated tau at the Thr212 site (p-Tau Thr212) with EC50 of 11.36 nM in Tau (P301L) 293T cells, EC50 of 16.99 nM in unstimulated, fast-dividing SH-SY5Y cells.
ZJCK-6-46 (20 mg/kg, 30 mg/kg) improved OA-induced cognitive dysfunction by reducing the expression level of phosphorylated tau in OA-induced AD mouse models.
| M.Wt | 395.47 | |
| Formula | C24H21N5O | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
10 mM in DMSO |
|
1. Huanhua Chen, et al. J Med Chem. 2024 Jul 23. doi: 10.1021/acs.jmedchem.4c00483.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
