Application In Synthesis of 8-Bromooctanoic acid. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 8-Bromooctanoic acid, is researched, Molecular C8H15BrO2, CAS is 17696-11-6, about Discovery of selective CDK9 degraders with enhancing antiproliferative activity through PROTAC conversion. Author is Qiu, Xiaqiu; Li, Yuanqing; Yu, Bin; Ren, Jie; Huang, Huidan; Wang, Min; Ding, Hong; Li, Zhiyu; Wang, Jubo; Bian, Jinlei.
Cyclin-dependent kinase 9 (CDK9) is an increasingly important potential cancer treatment target. Nowadays, developing selective CDK9 inhibitors has been extremely challenging as its ATP-binding sites are similar with other CDKs. Here, we report that the CDK9 inhibitor BAY-1143572 is converted into a series of proteolysis targeting chimeras (PROTACs) which leads to several compounds inducing the degradation of CDK9 in acute myeloid leukemia cells at a low nanomolar concentration In addition, the most potent PROTAC mol. could inhibit cell growth more effectively than warhead alone, with little inhibition of other kinases. This enhanced antiproliferative activity is mediated by a slight increase in kinase inhibitory activity and an increase in the level of apoptosis induction. Moreover, the most potent PROTAC mol. could induce the degradation of CDK9 in vivo. Our work provides evidence that the most potent PROTAC mol. represents a lead for further development and that CDK9 degradation is a potential valuable therapeutic strategy in acute myeloid leukemia.
《Discovery of selective CDK9 degraders with enhancing antiproliferative activity through PROTAC conversion》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(8-Bromooctanoic acid)Application In Synthesis of 8-Bromooctanoic acid.
Reference:
Bromide – Wikipedia,
bromide – Wiktionary