DYRK1-IN-1 is a highly selective and ligand-efficientDYRK1Ainhibitor. DYRK1-IN-1 inhibitsDYRK1Aphosphorylation activity with anIC₅₀value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrantDYRK1Achemical probe^[1].

DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC₅₀value of 220 nM. DYRK1-IN-1 inhibits tau phosphorylation with an IC₅₀value 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 IC₅₀of 434 nM compared to the enzymatic IC₅₀of 75 nM^[1].

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

240.26

Solid

C₁₂H₁₂N₆

Room temperature in continental US; may vary elsewhere.

DMSO : 25 mg/mL(104.05 mM;ultrasonic and warming and heat to 60℃)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (10.41 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (10.41 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。