MELK-In-30e

MELK-In-30e (also known as 30e or MELKi-30e) is a novel, second-generation, highly potent, and selective small-molecule inhibitor of maternal embryonic leucine zipper kinase (MELK). Developed by researchers at the University of Texas MD Anderson Cancer Center and the University of Texas at Austin, MELK-In-30e acts as a slow-binding, ATP-competitive inhibitor of MELK. MELK is a protein kinase frequently overexpressed in aggressive breast cancers, including triple-negative breast cancer (TNBC) and inflammatory breast cancer (IBC), where it promotes cancer stem cell (CSC) maintenance, epithelial-mesenchymal transition (EMT), and metastasis. Preclinical studies have demonstrated that MELK-In-30e significantly suppresses tumor growth, reduces cancer cell motility and invasion, and decreases the expression of fibronectin (FN1) and proliferative markers like Ki-67. When combined with standard-of-care agents such as eribulin, MELK-In-30e shows enhanced tumor regression and improved survival in TNBC and IBC xenograft models.

Other names

MELK inhibitor 30eMELKi 30eMELKi30eMELKi-30e