HCI-2184

HCI-2184 is a novel, reversible small molecule inhibitor of Never in mitosis gene A-related kinase 2 (Nek2), a serine/threonine kinase associated with centrosome function and cell cycle progression. Developed by researchers at the Huntsman Cancer Institute, HCI-2184 was identified as a potent inhibitor with an IC50 range of 13-38 nM. Nek2 overexpression is linked to increased proteasome activity and resistance to bortezomib in multiple myeloma. By inhibiting Nek2, HCI-2184 reduces proteasome function, increases levels of cyclin B1 and cdc2, and induces cell cycle arrest in the G2/M phase. It has shown potential in sensitizing bortezomib-resistant multiple myeloma cells and inhibiting growth in various cancer cell lines, including lung cancer.