SGC-GAK

SGC-GAK is a potent and selective small molecule inhibitor of Cyclin G-associated kinase (GAK), developed as a chemical probe by the Structural Genomics Consortium (SGC). GAK is a member of the numb-associated kinase (NAK) family and plays a critical role in clathrin-mediated endocytosis and mitosis. In the context of oncology, GAK inhibition has been identified as a synthetic lethal vulnerability in FBXW7-deficient contexts, such as TAL1-driven T-cell acute lymphoblastic leukemia (T-ALL). SGC-GAK is primarily used as a research tool to study GAK biology and its potential as a therapeutic target in cancers characterized by FBXW7 mutations or TAL1 activation.