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DYRK1-IN-1
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
DYRK1-IN-1图片
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
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。
分子式C12H12N6
分子量240.26
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.