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。

DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC 50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe.

Solid

DYRK1A 220 nM (IC50) DYRK1A 3 nM (Kd)pa

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. has not independently confirmed the accuracy of these methods. They are for reference only.

DYRK1-IN-1 (1 mg/kg; i.v.) shows high clearance. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Sprague?Dawley rats

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

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

In Vitro: DMSO : 25 mg/mL (104.05 mM; ultrasonic and warming and heat to 60°C)配制储备液