ros-234

ROS 234 dioxalate is a potent antagonist of H3(pKB of 9.46 for Guinea-pig ileum H3-receptor)

ROS 234 is a highly effective H3 antagonist, demonstrating a strong binding affinity (pK B) of 9.46 for the Guinea-pig ileum H3 receptor and a pKi of 8.90 for the Rat cerebral cortex H3 receptor. Additionally, it exhibits an ex vivo ED50 of 19.12 mg/kg (ip) in the Rat cerebral cortex. It should be noted that ROS 234 demonstrates limited central access, as reported in [1] and [2].

BC13 是一种 CDK6/BRD4 抑制剂，对 CDK6 和 BRD4 的 IC50 值分别为 234 nM 和 36 nM。它显示出抗增殖活性，并可诱导细胞凋亡 (apoptosis) 和 DNA 损伤。BC13 还会导致 ROS 水平升高。