BMS-986176_product_DataBase

Bioactivity	BMS-986176 (LX-9211) is a highly selective, brain-penetrant, potent AAK1 (adaptor associated kinase 1) inhibitor with an IC50 of 2 nM. BMS-986176 can be used for neurodegenerative diseases research[1].
Target	IC50: 2 nM (AAK1)
Invitro	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[1].
Name	BMS-986176
CAS	1815613-42-3
Formula	C19H23F4N3O
Molar Mass	385.40
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Reference	[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.

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