BAY-320

BAY-320 is a selective and ATP-competitive Bub1 inhibitor that inhibits the kinase activity of Bub1 with an IC₅₀ of 680 nM. BAY-320 inhibits endogenous Bub1-mediated Sgo1 localization. BAY-320 affects cellular mitotic chromosome arrangement and spindle assembly. BAY-320 inhibits cell proliferation. BAY-320 can be used in the study of cancer such as ovarian cancer and cervical cancer^[1][2]. IC50 & Target:IC₅₀: 680 nM (human Bub1, 2 mM ATP)^[1] In Vitro:BAY-320 (0.01-10 μM, 20 min) effectively inhibits the phosphorylation of Bub1 substrate H2ApT120 with an IC₅₀ of 0.56 µM ^[1].
BAY-320 (10 μM-1 mM) inhibits Bub1 kinase activity with an IC₅₀ of 0.56 μM^[1].
BAY-320 (10 μM, 3 h) prevents the distribution of H2ApT120 along chromosome arms in tetracycline-induced cells and inhibits Bub1C fusion^[1].
BAY-320 (10 μM, 3 d) significantly prolongs the time required for DLD-1 cells to complete mitosis^[1].
BAY-320 (0-12.5 μM, 3 d) reduces colony formation in three cell lines: ovarian cancer cell lines (OVCAR-3), Kuramochi, and non-transformed RPE1 cell lines with a concentration of 10 μM^[1].
BAY-320 (0.25-10 μM, 30 min) demonstrates inhibition of Bub1 through Bub1 autophosphorylation and phosphorylation of histone H2A and T120^[2].
BAY-320 (3-10 μM, 14 h) achieves near-maximal inhibition of Bub1 and drastically reduces T120 phosphorylation in RPE1 and HeLa cells^[2].
BAY-320 (3 μM, 48 h) provokes at most minor effects on mitotic progression, which is marked by a short delay of anaphase onset in HeLa cells^[2].
BAY-320 (10 μM, 3 h) reduces the centromeric levels of Sgo1 and Sgo2 to ~20% of control values in RPE1 cells^[2].
BAY-320 (3 μM, 10 h) partially displaces all CPC subunits examined from centromeres in HeLa cells^[2].
BAY-320 (3 μM, 2 h) does not detectably affect the phosphorylation of the Haspin substrate histone H3 (T3) in HeLa S3 cells^[2].
BAY-320 (3 μM, 24 h) lowers the percentage of HeLa cells maintaining a SAC arrest from 17% to 4% and 2% in response to Bub1 inhibition^[2].