inh154

INH154 is a **novel, potent small molecule inhibitor** that disrupts the interaction between Hec1 and Nek2, two proteins critical for mitosis and chromosome segregation in tumor cells. Mechanistically, INH154 binds to Hec1, forming a "death-trap" that leads to Nek2 degradation, suppression of Hec1 S165 phosphorylation, and ultimately apoptotic cell death in cancer cells. In vitro studies report IC50 values of 0.20 µM (HeLa cells) and 0.12 µM (MDA-MB-468 breast cancer cells), while in vivo preclinical studies demonstrate significant inhibition of tumor growth and proliferation in mouse models, with a lack of noteworthy toxicity. INH154 is distinguished from newer NEK2 inhibitors (e.g., NBI-961) by its indirect mechanism, as it does not prevent NEK2 autophosphorylation or proteasomal degradation in diffuse large B-cell lymphoma, but is potent in models with co-elevated Nek2 and Hec1, making it primarily an experimental targeted cancer therapy[1][4][7][9][10].

Other names

INH154INH-154INH 154