Mps-BAY1

Mps-BAY1 is a potent, small-molecule inhibitor of Monopolar Spindle 1 (MPS1), also known as TTK protein kinase, which is a critical mitotic kinase overexpressed in various human cancers. Developed by Bayer, Mps-BAY1 selectively inhibits MPS1 with low nanomolar potency, leading to the inactivation of the spindle assembly checkpoint (SAC) and disruption of chromosome alignment during metaphase. This mechanism causes cells to enter anaphase prematurely, resulting in severe chromosome missegregation, aneuploidy, and polyploidization. Ultimately, these mitotic perturbations trigger cell death via the intrinsic pathway of apoptosis. Preclinical studies have demonstrated that Mps-BAY1 exhibits significant antineoplastic activity as a standalone agent and shows synergistic effects when combined with microtubule-targeting agents like paclitaxel, particularly in cervical cancer xenograft models.