717915-17-8Relevant articles and documents
Design, synthesis and biological evaluation of nuclear receptor-degradation inducers
Itoh, Yukihiro,Kitaguchi, Risa,Ishikawa, Minoru,Naito, Mikihiko,Hashimoto, Yuichi
, p. 6768 - 6778 (2012/01/13)
Compounds that regulate the function(s) of nuclear receptors (NRs) are useful for biological studies and as candidate therapeutic agents. Most such compounds are agonists or antagonists. On the other hand, we have developed specific protein degradation in
Inhibition of protein kinase C-driven nuclear factor-κB activation: Synthesis, structure-activity relationship, and pharmacological profiling of pathway specific benzimidazole probe molecules
Peddibhotla, Satyamaheshwar,Shi, Ranxin,Khan, Pasha,Smith, Layton H.,Mangravita-Novo, Arianna,Vicchiarelli, Michael,Su, Ying,Okolotowicz, Karl J.,Cashman, John R.,Reed, John C.,Roth, Gregory P.
supporting information; experimental part, p. 4793 - 4797 (2010/10/19)
A unique series of biologically active chemical probes that selectively inhibit NF-κB activation induced by protein kinase C (PKC) pathway activators have been identified through a cell-based phenotypic reporter gene assay. These 2-aminobenzimidazoles represent initial chemical tools to be used in gaining further understanding on the cellular mechanisms driven by B and T cell antigen receptors. Starting from the founding member of this chemical series 1a (notated in PubChem as CID-2858522), we report the chemical synthesis, SAR studies, and pharmacological profiling of this pathway-selective inhibitor of NF-κB activation.