BAY-1816032

BAY-1816032 (CAS No.: 1891087-61-8) is a synthetic benzimidazole small-molecule chemical probe that selectively inhibits the mitotic checkpoint serine/threonine kinase BUB1; this target plays a central regulatory role in kinetochore signaling, chromosome alignment, and the spindle assembly checkpoint, and therefore this product is mainly used for target validation and mechanistic studies in cell cycle research, cancer biology, and chemical biology. In biochemical and cellular systems, it exhibits potent and stable targeted binding to and inhibition of BUB1, with overall in vitro activity at the nanomolar level, and can inhibit phosphorylation of the classical BUB1 substrate histone H2A at Thr120 under cellular conditions; meanwhile, it maintains high selectivity across kinase panels, with non-target kinases generally showing activity only in the multi-micromolar range, such as distant kinases including FLT3. When used in combination with mitotic stress factors (such as paclitaxel), it can enhance phenotypes such as chromosome segregation defects during mitosis, helping to elucidate pathway dependence and support rational combination screening; inhibition of cell proliferation can be observed in human cell models from multiple origins, with effects mostly seen in the low micromolar range. Typical applications include quantitative evaluation of BUB1 signaling pathway activity, regulation of mitotic progression in cultured cells, high-content imaging or viability-based screening, and investigation of pathway dependence and tumor-related biological dynamics in in vivo models in research animals; the specific concentration or dose used in experiments is usually optimized and determined according to the research objective and experimental design.