DYRK1-IN-1

DYRK1-IN-1 是一种高度选择性和配体高效的 DYRK1A 抑制剂。DYRK1-IN-1 抑制DYRK1A 磷酸化活性，IC50 值为220 nM。DYRK1-IN-1 可用于研究中枢神经系统渗透 DYRK1A 化学探针。

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库存: 现货

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5mg

￥2062.00

1650.00

- +
10mg

￥3487.00

2790.00

- +
25mg

￥7012.00

5610.00

- +
50mg

￥11337.00

9070.00

- +

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Background

DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe[1].

DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 inhibits tau phosphorylation with an IC50 value of 0.59 μM. DYRK1-IN-1 exhibits good permeability and cellular activity without P-glycoprotein liability. DYRK1-IN-1 has good physicochemical properties and has demonstrated high levels of enzymatic potency, favorable aqueous solubility, exquisite kinome selectivity, and promising on-target in vitro inhibition. DYRK1-IN-1 (HEK293 cells) demonstrates acceptable cellular activity, with IC50 of 434 nM compared to the enzymatic IC50 of 75 nM[1].

DYRK1-IN-1 (1 mg/kg; i.v.) shows high clearance[1].

[1]. Henderson SH, et al. Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors. J Med Chem. 2021;64(15):11709-11728.