Tran, Kim T. published the artcileA Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity, HPLC of Formula: 1799973-82-2, the publication is Journal of Medicinal Chemistry (2019), 62(17), 8028-8052, database is CAplus and MEDLINE.
Inhibiting the protein-protein interaction (PPI) between the transcription factor Nrf2 and its repressor protein Keap1 has emerged as a promising strategy to target oxidative stress in diseases, including central nervous system (CNS) disorders. Numerous non-covalent small-mol. Keap1-Nrf2 PPI inhibitors have been reported to date, but many feature suboptimal physicochem. properties for permeating the blood-brain barrier, while others contain problematic structural moieties. Here, we present the first side-by-side assessment of all reported Keap1-Nrf2 PPI inhibitor classes using fluorescence polarization, thermal shift assay, and surface plasmon resonance-and further evaluate the compounds in an NQO1 induction cell assay and in counter tests for nonspecific activities. Surprisingly, half of the compounds were inactive or deviated substantially from reported activities, while we confirm the cross-assay activities for others. Through this study, we have identified the most promising Keap1-Nrf2 inhibitors that can serve as pharmacol. probes or starting points for developing CNS-active Keap1 inhibitors.
Journal of Medicinal Chemistry published new progress about 1799973-82-2. 1799973-82-2 belongs to triazoles, auxiliary class Other Aromatic Heterocyclic,Bromide,Ether, name is 5-Bromo-7-methoxy-1-methyl-1H-benzo[d][1,2,3]triazole, and the molecular formula is C4H3Cl2N3, HPLC of Formula: 1799973-82-2.
Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics