758679-97-9

Usage

Uses

Used in Pharmaceutical Industry:
CID-2858522 is used as a pharmaceutical compound for its ability to selectively inhibit the antigen receptor-mediated NF-κB activation pathway. This inhibition can be beneficial in treating conditions where the NF-κB pathway is overactive or dysregulated, such as in inflammatory diseases or certain types of cancer.
Used in Research Applications:
In the field of research, CID-2858522 serves as a valuable tool for studying the role of NF-κB in various cellular processes. By selectively inhibiting this pathway, researchers can gain insights into the molecular mechanisms underlying different diseases and potentially identify new therapeutic targets.
Used in Drug Development:
CID-2858522's selective inhibition of the NF-κB pathway makes it a promising candidate for the development of new drugs targeting this pathway. Its potential applications in treating inflammatory diseases and cancer make it an attractive starting point for the design and synthesis of novel therapeutic agents.

Biochem/physiol Actions

CID2858522 specifically inhibits NF-kB activation downstream of protein kinsase C (PKC). CID2858522 dose dependently inhibits NF-kB reporter activity in PMA-ionomycin stimulated HEK293 cells, but does not affect NF-kB activity in cells challenged with TNFa, retinoic acid, or stimulation of the toll-like receptor signaling pathway.

Upstream product

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• 1189164-12-2 2-bromo-5,6-dimethyl-1H-benzo[d]imidazole 

Downstream Products

• 1135306-30-7 3-((1-(2-(3,5-di-tert-butyl-4-hydroxyphenyl)-2-oxoethyl)-5,6-dimethyl-1H-benzo[d]imidazol-2-yl)amino)propyl hept-6-ynoate 

Relevant academic research and scientific papers

Synthesis and physicochemical characterization of novel phenotypic probes targeting the nuclear factor-kappa B signaling pathway

Activation of nuclear factor-kappa B (NF-κB) and related upstream signal transduction pathways have long been associated with the pathogenesis of a variety of inflammatory diseases and has recently been implicated in the onset of cancer. This report provi

Inhibition of protein kinase C-driven nuclear factor-κB activation: Synthesis, structure-activity relationship, and pharmacological profiling of pathway specific benzimidazole probe molecules

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.

Selective benzimidazole inhibitors of the antigen receptor-mediated NF-κB activation pathway

Dysregulated antigen receptor-mediated NF-κB activation can contribute to development of autoimmunity, chronic inflammation, and malignancy. A chemical biology screening strategy has identified a substituted benzimidazole that selectively inhibits antigen receptor-mediated NF-κB activation without blocking other NF-κB activation pathways. A library of analogs was synthesized and the structure-activity relationship and metabolic stability for the series is presented.

INHIBITORS OF ANTIGEN RECEPTOR-INDUCED NF-kappa B ACTIVATION

A method to identify selective inhibitors of antigen receptor-mediated NF-κB activation is provided, as well as compositions having one or more of those inhibitors and methods of using those inhibitors.