BAY-1816032 is a benzimidazole budding inhibition relieved homolog protein 1 kinase (BUB1) inhibitor with IC50 of 0.7 nM and is orally active and abolishes nocodazole-induced Thr-120 phosphorylation of histone H2A, a major BUB1 target protein, in HeLa cells with IC50 of 29 nM.

BUB1 kinase:7 nM

METHODS: BAY-1816032 (0, 1.5625, 3.125, 6.25, 12.5, 25, 50 μM, 48 hours) treated ATC cells (TPC-1, 8505C), and CCK-8 assay was used to study cell viability.
RESULTS BAY-1816032 treatment resulted in a decrease in ATC cell viability, with IC50 values ​​of 4.230 μM in TPC-1 cells and 6.216 μM in 8505C cells. [2]
METHODS: Colony formation assay, cell cycle, invasion, migration and wound healing assay were performed after ATC cells were treated with BAY-1816032 (0, 2.5, 5 μM).
RESULTS BAY-1816032 can significantly reduce colony formation ability; BAY-1816032 can cause cell cycle arrest similar to siRNA; BAY-1816032 treatment can significantly hinder the invasion and migration of ATC cells in a dose-dependent manner. [2]

METHODS: BAY-1816032 (100 mg/kg, oral, 24 days) was used to treat 8505C xenograft model mice to evaluate the anti-ATC activity and safety of BAY-1816032 in mice.
RESULTS There was no significant difference in the body weight of each group of mice; the tumor weight of mice treated with BAY-1816032 was significantly reduced. [2]