OTS514 HCl

OTS514 HCl (CAS No.: 2319647-76-0) is a synthetic small-molecule, selective protein kinase inhibitor for biomedical research and drug discovery workflows, specifically targeting T-LAK cell-originated protein kinase (PDZ-binding kinase, PBK/TOPK), a mitotic MAPKK-like serine/threonine kinase that plays key roles in chromatin dynamics regulation, cytokinesis, and G2/M-phase progression, and shows elevated expression in research models derived from multiple tumor types; it is therefore commonly used in pathway-focused tumor biology and kinase signaling studies. Obtained through small-molecule screening and optimization, OTS514 shows low-nanomolar inhibitory activity against TOPK at the biochemical level (IC50 approximately 2.6 nM), and can effectively inhibit TOPK activity in cellular systems, producing phenotypes consistent with disruption of the mitotic program, including inhibition of proliferation, G2/M-phase arrest, and programmed cell death; its in vitro activity effects are typically in the nanomolar to submicromolar range. Mechanistically, TOPK has been shown to directly participate in mitotic chromosome remodeling and mediate phosphorylation of histone H3 at Ser10, while also cross-linking with broader MAPK signaling nodes; therefore, OTS514 is often used as a chemical biology probe to dissect TOPK-dependent regulation of mitotic checkpoints and downstream pathway readouts. Typical applications include cell viability and colony formation assays, flow cytometry-based cell cycle profiling, assessment of apoptosis markers, and immunoblotting or imaging analyses targeting TOPK substrates, such as phosphorylated histone H3; in animal studies, it may also be used in xenograft models to evaluate target occupancy and signaling consequences, with experimental concentrations or doses typically determined by the specific study design and objectives. This product is intended only for laboratory research related to kinase biology, target validation, and drug development, and is not for human or veterinary use or any non-research application.