2. Signaling Pathways
  3. Neuronal Signaling
  4. AAK1

AAK1

Adaptor-associated Kinase 1; AP2-associated kinase 1

Adaptor-associated kinase 1 (AAK1), also known as AP2-associated kinase 1, is a 104 kDa serine/threonine kinase. AAK1 is expressed within the cell in the membrane and cytoplasm. It is a key endocytic kinase that is known to have two physiological substrates. AAK1 binds and phosphorylates the threonine residue at position 102 of the Numb protein. AAK1-mediated phosphorylation has been shown to be important for the endocytic activity of Numb. AAK1 is also an interacting partner of the adaptor protein 2 (AP2) complex and AAK1 recruits AP-2 to the plasma membrane. Phosphorylation of the threonine residue in the µ–subunit of AP2 (AP2M1) by AAK1 increases its binding affinity for specific tyrosine- or dileucine-based sorting signals of certain membrane receptors. It enhances cargo recruitment, vesicle assembly, and efficient internalization. AAK1 is also implicated in the regulation of various signaling pathways, such as the Notch pathway. It has been shown that AAK1 directly interacts with ligand activated Notch, but not with the inactive fulllength receptor.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-161261
    SARS-CoV-2-IN-81
    		Inhibitor
    SARS-CoV-2-IN-81 (compound 12e) is a potent AAK1 inhibitor with an IC50 value of 9.38 nM. SARS-CoV-2-IN-81 shows anti-viral property against SARS-CoV-2. SARS-CoV-2-IN-81 attenuates AAK1-induced phosphorylation of AP2M1 threonine 156 and disrupts the direct interaction between AP2M1 and ACE2, ultimately inhibiting SARS-CoV-2 infection.
    SARS-CoV-2-IN-81
  • HY-159931
    HW161023
    		Inhibitor
    HW161023 (compound 5) is an orally active AP2-associated protein kinase 1 (AAK1) inhibitor with IC50 values of 5.4 nM and 11.9 μM aganist of AAK1and hERG, respectively. HW161023 inhibits the pain in chronic constriction injury of the sciatic nerve rat model.
    HW161023
  • HY-176706
    AAK1-IN-10
    		Inhibitor
    AAK1-IN-10 (Compound 1-2) is an AAK1 inhibitor. AAK1-IN-10 has significant AAK1 enzyme inhibitory activity (IC50: 9.62 nM). AAK1-IN-10 mainly exerts its effects by inhibiting the activity of connexin-associated kinase 1 (AAK1). AAK1-IN-10 has low cardiotoxicity (IC50 = 13.7 μM). AAK1-IN-10 can be used in the study of diabetic neuropathy and postherpetic pain.
    AAK1-IN-10
  • HY-162388
    TIM-098a
    		Inhibitor
    TIM-098a is a selective AAK1 inhibitor with an IC50 of 0.24 µM. TIM-098a has no inhibitory activity against CaMKK isoforms. TIM-098a inhibits AAK1-regulated endocytosis by suppressing AAK1 kinase activity.
    TIM-098a
  • HY-144301
    AAK1-IN-2
    AAK1-IN-2 (compound (S)-31) is a potent, selective and brain-penetrant inhibitor of Adaptor Protein 2-Associated Kinase 1 (AAK1), with an IC50 of 5.8 nM. AAK1-IN-2 can be used for the research of neuropathic pain.
    AAK1-IN-2
  • HY-147083
    SGC-AAK1-1N
    		Inhibitor
    SGC-AAK1-1N is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor, with an IC50 of 1.8 μM.
    SGC-AAK1-1N
  • HY-101290
    BMT-090605
    		Inhibitor 98.27%
    BMT-090605 is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 value of 0.6 nM. BMT-090605 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 45 nM and 60 nM, respectively. BMT-090605 can be used for the research of neuropathic pain.
    BMT-090605
  • HY-145839
    AAK1-IN-5
    AAK1-IN-5 is a highly selective, CNS-penetrable, and orally active adaptor protein-2-associated kinase 1 (AAK1) inhibitor (AAK1 IC50 of 1.2 nM, Filt Ki of 0.05 nM, and cell IC50 of 0.5 nM). AAK1-IN-4 has the potential for the research for neuropathic pain.
    AAK1-IN-5
  • HY-159879
    AAK1-IN-6
    		Inhibitor
    AAK1-IN-6 (Compound 23) is an inhibitor of AP-2-associated protein kinase 1 (AAK1, IC50 = 12 nM) with antiviral activity against the dengue virus (DNEV2, EC50 = 0.24 μM) and Venezuelan equine encephalitis virus (VEEV, EC50 = 0.30 μM). AAK1-IN-6 can be utilized in antiviral research.
    AAK1-IN-6
  • HY-120092
    BMT-046091
    		Inhibitor
    BMT-046091 is a selective inhibitor of adaptor-associated kinase 1 (AAK1). BMT-046091 inhibits phosphorylation of the μ2 peptide by AAK1 with an IC50 value of 2.8 nM.
    BMT-046091
Cat. No. Product Name / Synonyms Application Reactivity