BMS-986176 (LX-9211) 是一种有效的，高选择性、可穿过血脑屏障的 AAK1 (adaptor associated kinase 1) 抑制剂，IC₅₀ 为 2 nM。BMS-986176 可用于神经退行性疾病的研究。

BMS-986176 (LX-9211) is a highly selective, brain-penetrant, potent AAK1 (adaptor associated kinase 1) inhibitor with an IC 50 of 2 nM. BMS-986176 can be used for neurodegenerative diseases research.

Solid

IC50: 2 nM (AAK1)

Adaptor associated kinase 1 (AAK1) is a member of the Arkl/Prkl family of serine/threonine kinases. AAKl mRNA exists in two splice forms termed short and long. The long form predominates and is highly expressed in brain and heart. AAKl is enriched in synaptosomal preparations and is co-localized with endocytic structures in cultured cells. AAKl modulates clatherin coated endocytosis, a process that is important in synaptic vesicle recycling and receptor-mediated endocytosis. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

[1]. Guanglin Luo, et al. Biaryl kinase inhibitors. WO2015153720A1.
[2]. Guanglin Luo, et al. Discovery of ( S)-1-((2,6-Bis(difluoromethyl)-[2,4-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): A Highly Selective, CNS Penetrable, and Orally Active Adaptor Protein-2 Associated Kinase 1 Inhibitor in Clinical Trials for the Treatment of Neuropathic Pain. J Med Chem. 2022 Mar 24;65(6):4457-4480.

In Vitro: DMSO : 220 mg/mL (570.84 mM; Need ultrasonic)配制储备液