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。