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AAK1-IN-3

Names

[ CAS No. ]:
1802703-20-3

[ Name ]:
AAK1-IN-3

Biological Activity

[Description]:

AAK1-IN-3, a quinoline analogue, is a brain-penetrant adaptor protein 2-associated kinase 1 (AAK1) inhibitor with an IC50 of 11 nM. AAK1-IN-3 has the potential for neuropathic pain research[1].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Neurological Disease

[In Vitro]

AAK1-IN-3 (compound (R)-31) is brain-penetrant kinase inhibitors with a B/P ratio of 1.3[1]. AAK1-IN-3 inhibits AAK1 in HEK293 cells (IC50=108 nM)[1].

[In Vivo]

AAK1-IN-3 (compound (R)-31; 30 mg/kg; sc; signle dose) causes a 46% reduction of μ2 phosphorylation in C57BL6 mice[1].

[References]

[1]. Richard A Hartz, et al. Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2-Associated Kinase 1 Inhibitors. J Med Chem. 2022 Mar 10;65(5):4121-4155.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H20N4

[ Molecular Weight ]:
316.40

Related Compounds