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-117626
    LP-935509
    		Inhibitor 99.74%
    LP-935509 is an orally active, potent, selective, ATP-competitive and brain-penetrant inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 shows antinociceptive activity. LP-935509 can be used for neuropathic pain and SARS-CoV-2 research.
    LP-935509
  • HY-134829
    BMS-986176
    		98.79%
    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.
    BMS-986176
  • HY-120179
    LP-922761
    		98.21%
    LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors.
    LP-922761
  • HY-123940
    SGC-AAK1-1
    		98.93%
    SGC-AAK1-1 is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor with an IC50 of 270 nM and a Ki of 9 nM. SGC-AAK1-1 also potently inhibits BMP2K. SGC-AAK1-1 is used to study Wnt pathway related to AAK1.
    SGC-AAK1-1
  • HY-148062
    RSS0680
    		98.03%
    RSS0680 (Example 22) is a bifunctional compound targeted protein degradation of kinases. RSS0680 degrades AAK1, CDK1, CDK16, CDK2, CDK4, CDK6, EIF2AK4, GAK, LATSl, LIMK2, MAPK6, MAPKAPK5, MARK2, MARK4, MKNK2, NEK9, RPS6KB1, SIK2, SNRK, STK17A, STK17B, STK35, and WEEl. RSS0680 can be used for research of disease or disorder mediated by aberrant kinase activity.
    RSS0680
  • 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
  • HY-115868
    BMS-911172
    		98.46%
    BMS-911172 is an adaptor associated kinase 1 (AAK1 kinase) inhibitor (IC50 = 35 nM).
    BMS-911172
  • HY-148063
    DB0614
    		98.80%
    DB0614 is a PROTAC based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2 and ULK1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity.(Blue: Thalidomide-4-OH (HY-103596), Black: linker, Pink: FLT3-IN-17 (HY-148070))
    DB0614
  • HY-101290A
    BMT-090605 hydrochloride
    		Inhibitor 99.09%
    BMT-090605 hydrochloride is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 value of 0.6 nM. BMT-090605 hydrochloride shows antinociceptive activity. BMT-090605 hydrochloride 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 hydrochloride can be used for the research of neuropathic pain.
    BMT-090605 hydrochloride
  • HY-120179A
    LP-922761 hydrate
    		≥98.0%
    LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors.
    LP-922761 hydrate
  • HY-117453
    BMS-901715
    BMS-901715 is a potent and selective adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 of 3.3 nM.
    BMS-901715
  • HY-144301A
    AAK1-IN-2 TFA
    AAK1-IN-2 TFA (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 TFA can be used for the research of neuropathic pain.
    AAK1-IN-2 TFA
  • HY-144302
    AAK1-IN-3
    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.
    AAK1-IN-3
  • HY-145838
    AAK1-IN-4
    AAK1-IN-4 is a highly selective, CNS-penetrable, and orally active adaptor protein-2-associated kinase 1 (AAK1) inhibitor (AAK1 IC50 of 4.6 nM, Filt Ki of 0.9 nM, and cell IC50 of 8.6 nM). AAK1-IN-4 has the potential for the research for neuropathic pain.
    AAK1-IN-4
  • 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-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-135871
    BMT-124110
    BMT-124110 is a potent, selective AAK1 inhibitor with an IC50 of 0.9 nM. BMT-124110 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 17 and 99 nM, respectively.
    BMT-124110
  • 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
Cat. No. Product Name / Synonyms Application Reactivity