Fang, Zhen; Liu, Yang; Zhang, Rong; Chen, Qiang; Wang, Tianqi; Yang, Wei; Fan, Yan; Yu, Chundong; Xiang, Rong; Yang, Shengyong published an article in 2021. The article was titled 《Discovery of a potent and selective inhibitor of histone lysine demethylase KDM4D》, and you may find the article in European Journal of Medicinal Chemistry.Reference of 2-Pyridinylboronic acid The information in the text is summarized as follows:
Histone lysine demethylase 4D (KDM4D) plays an important role in the regulation of tumorigenesis, progression and drug resistance and has been considered a potential target for cancer treatment. However, there is still a lack of potent and selective KDM4D inhibitors. In this investigation, we report a new class of KDM4D inhibitors containing the 2-(aryl(pyrrolidine-1-yl)methyl)phenol scaffold, identified through AlphaLisa-based screening, structural optimization, and structure-activity relationship analyses. Among these inhibitors, 24s (I) was the most potent, with an IC50 value of 0.023 ± 0.004μM. This compound exhibited more than 1500-fold selectivity towards KDM4D vs. KDM4A as well as other JMJD subfamily members, indicating good selectivity for KDM4D. Kinetic anal. indicated that 24s did not occupy the 2-oxoglutarate binding pocket. In an in vitro assay, 24s significantly suppressed the proliferation and migration of colorectal cancer (CRC) cells. Overall, this study has identified a good tool compound to explore the biol. function of KDM4D and a good lead compound for drug discovery targeting KDM4D. After reading the article, we found that the author used 2-Pyridinylboronic acid(cas: 197958-29-5Reference of 2-Pyridinylboronic acid)
2-Pyridinylboronic acid(cas: 197958-29-5) belongs to pyridine. Pyridines form stable salts with strong acids. Pyridine itself is often used to neutralize acid formed in a reaction and as a basic solvent. Reference of 2-Pyridinylboronic acid