INH1

INH1 is a small molecule inhibitor that targets the interaction between NIMA-related kinase 2 (NEK2) and the kinetochore protein Hec1 (also known as NDC80). NEK2 is a serine/threonine kinase that is frequently overexpressed in high-risk multiple myeloma (MM) and other cancers, where it plays a critical role in cell cycle regulation, centrosome duplication, and drug resistance. INH1 works by disrupting the Hec1-NEK2 interaction, which leads to the degradation of NEK2 and the subsequent inhibition of its downstream signaling pathways. Research indicates that NEK2 inhibition by INH1 can overcome drug resistance, reduce tumor growth in xenograft models, and enhance the efficacy of immune checkpoint blockades, such as PD-1/PD-L1 inhibitors, by modulating the EZH2-mediated epigenetic regulation of PD-L1. It is primarily used as a research tool compound to study NEK2 biology and its therapeutic potential in oncology.