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-144302A
    AAK1-IN-3 TFA
    AAK1-IN-3 TFA, 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.
    AAK1-IN-3 TFA
  • HY-169405
    AAK1/HDACs-IN-1
    		Inhibitor
    AAK1/HDACs-IN-1 (Compound 12) is the dual inhibitor for AAK1 and HDAC, that inhibits AAK1, HDAC1, and HDAC6 with IC50s of 15.9, 148.6, and 5.2 nM, respectively. AAK1/HDACs-IN-1 inhibits SARS-CoV-2 infection, suppresses the endocytosis of ACE2-SARS-CoV-2 complex, as well as AP2M1-ACE2 interaction.
    AAK1/HDACs-IN-1
  • 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-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-174213
    AAK1-IN-7
    		Inhibitor
    AAK1-IN-7 (Compound 16) is a dual AAK1/GAK inhibitor (EC50 values are 40 and 80 nM, respectively). AAK1-IN-7 inhibits the phosphorylation of AP2-µ2 subunit at T156. AAK1-IN-7 has weak antiviral activity against RNA viruses.
    AAK1-IN-7
  • HY-174214
    AAK1-IN-8
    		Inhibitor
    AAK1-IN-8 (Compound 18) is a pan-NAK inhibitor. AAK1-IN-8 inhibits AAK1 and GAK (EC50 values are 50 and 190 nM, respectively). AAK1-IN-8 inhibits the phosphorylation of AP2-µ2 subunit at T156.
    AAK1-IN-8
  • 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