HI-TOPK-032

HI-TOPK-032 is a small molecule inhibitor specifically targeting T-LAK cell-originated protein kinase (TOPK), also known as PDZ-binding kinase (PBK). It was developed primarily as a research tool to investigate the role of TOPK in oncogenesis and as a potential therapeutic agent for various malignancies. The drug exerts its effects by binding to TOPK and inhibiting its kinase activity, which prevents the phosphorylation of downstream substrates such as Y-box binding protein 1 (YB1). Disruption of the TOPK/YB1 axis leads to reduced transcription of genes like eukaryotic translation elongation factor 1 alpha 1 (eEF1A1), consequently inactivating the AKT/mTOR signaling pathway. Preclinical studies have shown that HI-TOPK-032 effectively suppresses cell proliferation, colony formation, and tumor growth in models of esophageal cancer, colon cancer, glioblastoma, and solar ultraviolet-induced skin carcinogenesis by inducing cell cycle arrest and apoptosis.