Regulates clathrin-mediated endocytosis by phosphorylating the AP2M1/mu2 subunit of the adaptor protein complex 2 (AP-2) which ensures high affinity binding of AP-2 to cargo membrane proteins during the initial stages of endocytosis. Isoform 1 and isoform 2 display similar levels of kinase activity towards AP2M1. Regulates phosphorylation of other AP-2 subunits as well as AP-2 localization and AP-2-mediated internalization of ligand complexes. Phosphorylates NUMB and regulates its cellular localization, promoting NUMB localization to endosomes. Binds to and stabilizes the activated form of NOTCH1, increases its localization in endosomes and regulates its transcriptional activity.
|SGC-AAK1-1 is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor.
|Pim1 AKK1-IN-1 is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively and also inhibits MPSK1 and TNIK.
|LP 922761 is a potent AAK1 inhibitor with IC50 of 4.8 and 7.6 nM in enzyme and cell assays, respectively.
|BMS-901715 is a potent and selective adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 of 3.3 nM.