GSK-923295

GSK-923295 is a first-in-class, small-molecule, allosteric inhibitor of the mitotic kinesin centromere-associated protein E (CENP-E). Developed through a collaboration between Cytokinetics and GlaxoSmithKline (GSK), it specifically targets CENP-E motor function, which plays an essential role in chromosome movement during mitosis and regulates the cell-cycle transition from metaphase to anaphase. By inhibiting CENP-E, GSK-923295 induces cell cycle arrest in mitosis with bipolar spindles and misaligned chromosomes, ultimately leading to apoptosis. Preclinical studies demonstrated broad antitumor activity against various human tumor xenografts including colon, breast, ovarian, and lung cancers. It was the first drug candidate to enter human clinical trials that specifically targets CENP-E and has reached Phase I clinical development for advanced solid tumors[1][2][3][4][5].

Other names

1088965-37-0