ZJCK-6-46 | DYRK1A inhibitor | Probechem Biochemicals

Chemical Structure : ZJCK-6-46

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ZJCK-6-46 (DYRK1A inhibitor)

货号: 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.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	395.47
分子式	C24H21N5O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-2-((6-(6-Methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)quinazolin-4-yl)amino)-2-phenylethan-1-ol

参考文献

1. Huanhua Chen, et al. J Med Chem. 2024 Jul 23. doi: 10.1021/acs.jmedchem.4c00483.