Vinyl bromides undergo the Heck reaction, which involves C-C coupling with alkene to give substituted alkenes. 4897-84-1, formula is C5H9BrO2, Name is Methyl 4-bromobutanoate. Methyl bromide is a precursor in the manufacture of several chemicals and is employed as a soil sterilant, mainly for seed production. Application of C5H9BrO2.
Roberts, Brett L.;Ma, Zhi-Xiong;Gao, Ang;Leisten, Eric D.;Yin, Dan;Xu, Wei;Tang, Weiping research published 《 Two-Stage Strategy for Development of Proteolysis Targeting Chimeras and its Application for Estrogen Receptor Degraders》, the research content is summarized as follows. Proteolysis targeting chimeras (PROTACs) have emerged as useful chem. probes and potential therapeutics by taking advantage of the ubiquitin-proteasome system to degrade intracellular disease-associated proteins. PROTACs are heterobifunctional mols. composed of a target protein ligand, E3 ubiquitin ligase ligand, and a linker between them. The generation of efficient PROTACs requires screening of many parameters, especially the lengths and types of the linkers. The authors report the proof-of-concept study using a two-stage strategy to facilitate the development of PROTACs against the estrogen receptor (ER). In stage one, a library of close to 100 PROTACs was synthesized by simply mixing a library of ERα ligands containing a hydrazide functional group at different positions with a preassembled library of E3 ligase ligands bearing different types and lengths of linkers with a terminal aldehyde group in a 1:1 ratio. Cell-based screening occurred without further purification, because the formation of the acylhydrazone linkage is highly efficient and produces water as the only byproduct. Compound A3 was the most potent ER degrader in two ER+ cell lines (DC50= ~10 nM, Dmax= ≥ 95%). Stage two involved transformation to a more stable amide linker to generate a more drug-like mol. The new compound, AM-A3, showed comparable biol. activity (DC50 = 1.1 nM, Dmax = 98%) and induced potent antiproliferation (IC50= 13.2 nM, Imax= 69%) in MCF-7. This proof-of -concept study demonstrates that the two-stage strategy can significantly facilitate the development of PROTACs against ER without the tedious process of making large numbers of PROTACs one by one. It has the potential to be expanded to many other targets.
4897-84-1, Methyl 4-bromobutyrate,also as known as 4-Bromobutyric acid methyl ester, is a useful research compound. Its molecular formula is C5H9BrO2 and its molecular weight is 181.03 g/mol. The purity is usually 95%.
4-Bromobutyric acid methyl ester is a synthetic compound that can be used to inhibit the activity of the G1 phase cyclin-dependent kinases. It has been shown to inhibit protein synthesis by alkylating the amino groups of proteins and fatty acids. 4-Bromobutyric acid methyl ester also inhibits the growth of cancer cell lines, such as renal carcinoma cells. The mechanism of action for this drug is not well understood, but it may be due to its ability to bind with monoclonal antibodies and enter kidney cells by passive diffusion., Application of C5H9BrO2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary