1. Signaling Pathways
  2. Neuronal Signaling
  3. AAK1


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.

AAK1 相关产品 (5):

目录号 产品名 作用方式 纯度
  • HY-117626
    LP-935509 Inhibitor 99.74%
    LP-935509 是一种口服有效的、选择性的、ATP 竞争性的和可透过血脑屏障的一种接头蛋白-2 相关激酶 1 (AAK1) 抑制剂,其 IC50 为 3.3 nM,Ki 为 0.9 nM。LP-935509 也是 BIKE 的有效抑制剂 (IC50=14 nM) 和 GAK 的中度抑制剂 (IC50=320 nM)。LP-935509 具有镇痛活性。LP-935509 可用于神经性疼痛和 SARS-CoV-2 的研究。
  • HY-115868
    BMS-911172 98.46%
    BMS-911172 是一种 AAK1 激酶抑制剂(IC50 = 35 nM)。
  • HY-148063
    DB1113 (Example 24) 是一种靶向蛋白激酶降解的双功能化合物。DB1113 可降解 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 和 ULK1。DB1113 可用于研究异常激酶活性介导的疾病或紊乱。
  • HY-147083
    SGC-AAK1-1N Inhibitor
    SGC-AAK1-1N 是一种有效且选择性的 AAK1 (AP2 相关激酶 1) 抑制剂,其 IC50 值为 1.8 μM。
  • HY-148062
    RSS0680 (Example 22) 是一种靶向蛋白降解激酶的双功能化合物。RSS0680 降解 AAK1、CDK1、CDK16、CDK2、CDK4、CDK6、EIF2AK4、GAK、LATSl、LIMK2、MAPK6、MAPKAPK5、MARK2、MARK4、MKNK2、NEK9、RPS6KB1、SIK2、SNRK、STK17A、STK17B、STK35 和 WEEl。RSS0680 可用于研究异常激酶活性介导的疾病或紊乱。