2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Cyclin G-associated Kinase (GAK)

Cyclin G-associated Kinase (GAK)

Auxilin 2

Cyclin G-associated kinase (GAK), also known as auxilin 2, is a cellular serine/threonine kinase. GAK was originally identified as an association partner of cyclin G and CDK5 (cyclin-dependent kinase 5). It is essential for clathrin trafficking, mediating binding of clathrin to the plasma membrane and the trans-Golgi network, and regulating receptor signalling by influencing trafficking downstream of clathrin-coated vesicles. GAK has been reported to phosphorylate the μ2 subunit of adaptor protein 1 and 2 (AP-1 and AP-2), thereby initiating a conformational change and enhancing their binding to sorting signals (in the form of tyrosineor dileucine-based motifs) within the cargo. In addition to its role in the cytoplasm, GAK has important functions in the nucleus. It is required for the maintenance of proper centrosome maturation and progression through mitosis. GAK plays a central role during development and GAK KO mice die early in gestation.

Cyclin G-associated Kinase (GAK) Related Products (26):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-178036
    ZM484
    		Inhibitor
    ZM484 is a potent dual p53-MDM2/TOP1 inhibitor that exhibits antiproliferative and antitumor activity both in vitro and in vivo. ZM484 effectively upregulates p53 and MDM2 proteins and maintains TOP1 inhibitory activity by the release of camptothecin (CPT) and a potent p53-MDM2 inhibitor. ZM484 induces cell cycle arrest and apoptosis by regulating the expression of key apoptosis- and cycle-related proteins, including caspase-3, Bcl-2, and Cyclin B1. ZM484 can be used for colorectal cancer research.
    ZM484
  • HY-119948
    AKCI
    		Modulator
    AKCI is a type of AURKC-IκBα interaction inhibitor, with an IC50 value of 24.9 μM. In MDA-MB-231 cells, AKCI can induce G2/M cell cycle arrest by regulating the p53/p21/CDC2/cyclin B1 pathway, inhibit cell migration and invasion, and reduce colony formation and tumor growth. AKCI can be used for research on breast cancer.
    AKCI
  • HY-101290AR
    BMT-090605 hydrochloride (Standard)
    		Inhibitor
    BMT-090605 (hydrochloride) (Standard) is the analytical standard of BMT-090605 (hydrochloride) (HY-101290A). This product is intended for research and analytical applications. 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 (Standard)
  • 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-181169
    GAK-IN-3
    		Inhibitor
    GAK-IN-3 is a cyclin G-associated kinase (GAK) inhibitor with an IC50 of 207 nM and a Ki of 66 nM. GAK-IN-3 inhibits kinase activity in the nanomolar range by binding to GAK’s ATP-binding site. GAK-IN-3 acts as a cytotoxic agent that reduces viability of Ewing sarcoma cells. GAK-IN-3 can be used for the research of ewing sarcoma.
    GAK-IN-3
  • 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