Organobromine compounds, also called organobromides, are organic compounds that contain carbon bonded to bromine. 4897-84-1, formula is C5H9BrO2, The most pervasive is the naturally produced bromomethane. Recommanded Product: Methyl 4-bromobutanoate
Kahl, Dylan J.;Hutchings, Kim M.;Lisabeth, Erika Mathes;Haak, Andrew J.;Leipprandt, Jeffrey R.;Dexheimer, Thomas;Khanna, Dinesh;Tsou, Pei-Suen;Campbell, Phillip L.;Fox, David A.;Wen, Bo;Sun, Duxin;Bailie, Marc;Neubig, Richard R.;Larsen, Scott D. research published 《 5-Aryl-1,3,4-oxadiazol-2-ylthioalkanoic Acids: A Highly Potent New Class of Inhibitors of Rho/Myocardin-Related Transcription Factor (MRTF)/Serum Response Factor (SRF)-Mediated Gene Transcription as Potential Antifibrotic Agents for Scleroderma》, the research content is summarized as follows. Through a phenotypic high-throughput screen using a serum response element luciferase promoter, we identified a novel 5-aryl-1,3,4-oxadiazol-2-ylthiopropionic acid lead inhibitor of Rho/myocardin-related transcription factor (MRTF)/serum response factor (SRF)-mediated gene transcription with good potency (IC50 = 180 nM). We were able to rapidly improve the cellular potency by 5 orders of magnitude guided by sharply defined and synergistic SAR. The remarkable potency and depth of the SAR, as well as the relatively low mol. weight of the series, suggests, but does not prove, that binding to the unknown mol. target may be occurring through a covalent mechanism. The series nevertheless has no observable cytotoxicity up to 100 μM. Ensuing pharmacokinetic optimization resulted in the development of two potent and orally bioavailable anti-fibrotic agents that were capable of dose-dependently reducing connective tissue growth factor gene expression in vitro as well as significantly reducing the development of bleomycin-induced dermal fibrosis in mice in vivo.
Recommanded Product: Methyl 4-bromobutanoate, 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., 4897-84-1.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary