Pyridine is a basic heterocyclic organic compound with the chemical formula C5H5N. It is structurally related to benzene, with one methine group (=CH−) replaced by a nitrogen atom. 16133-25-8, formula is C5H4ClNO2S, Name is Pyridine-3-sulfonyl chloride. It is a highly flammable, weakly alkaline, water-miscible liquid with a distinctive, unpleasant fish-like smell. Related Products of 16133-25-8.
Heightman, Tom D.;Callahan, James F.;Chiarparin, Elisabetta;Coyle, Joseph E.;Griffiths-Jones, Charlotte;Lakdawala, Ami S.;McMenamin, Rachel;Mortenson, Paul N.;Norton, David;Peakman, Torren M.;Rich, Sharna J.;Richardson, Caroline;Rumsey, William L.;Sanchez, Yolanda;Saxty, Gordon;Willems, Henriette M. G.;Wolfe, Lawrence;Woolford, Alison J.-A.;Wu, Zining;Yan, Hongxing;Kerns, Jeffrey K.;Davies, Thomas G. research published 《 Structure-Activity and Structure-Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein-Protein Interaction》, the research content is summarized as follows. The KEAP1-NRF2-mediated cytoprotective response plays a key role in cellular homoeostasis. Insufficient NRF2 signaling during chronic oxidative stress may be associated with the pathophysiol. of several diseases with an inflammatory component, and pathway activation through direct modulation of the KEAP1-NRF2 protein-protein interaction is being increasingly explored as a potential therapeutic strategy. Nevertheless, the physicochem. nature of the KEAP1-NRF2 interface suggests that achieving high affinity for a cell-penetrant druglike inhibitor might be challenging. We recently reported the discovery of a highly potent tool compound which was used to probe the biol. associated with directly disrupting the interaction of NRF2 with the KEAP1 Kelch domain. We now present a detailed account of the medicinal chem. campaign leading to this mol., which included exploration and optimization of protein-ligand interactions in three energetic “hot spots” identified by fragment screening. In particular, we also discuss how consideration of ligand conformational stabilization was important to its development and present evidence for preorganization of the lead compound which may contribute to its high affinity and cellular activity.
Related Products of 16133-25-8, Pyridine-3-sulfonyl chloride is a useful research compound. Its molecular formula is C5H4ClNO2S and its molecular weight is 177.61 g/mol. The purity is usually 95%.
Pyridine-3-sulfonyl chloride is a reagent used in the synthesis of pyrimidine derivatives with anti-proliferative activity against negative breast cancer cells.
Pyridine-3-sulfonyl chloride is a chemical compound that binds to the active site of cytochrome P450 enzymes. It can be used to study the effects of matrix effect on reaction solution. Pyridine-3-sulfonyl chloride has been shown to have an UV absorption spectrum with a maximum at 280 nm and a p450 activity that is proportional to the concentration of human serum. This compound has been shown to inhibit kinase domain in vitro assays, which may have clinical relevance in the treatment of obesity., 16133-25-8.