The NF-κB/Rel transcription factors, known to be involved in the regulation of pro-inflammatory cytokines and the pathogenesis of a variety of diseases, are present in the cytosol in an inactive state, complexed with inhibitory IκB proteins. NF-κB is activated upon degradation of IκB following IKK-α and IKK-β phosphorylation. IKK-ε, a homolog of IKKα and IKK-β, can also activate NF-κB. IKK-ε is expressed predominantly in immune cells, and is thought to play a role in the immune response. CAY10576 is a benzimidazole analog that selectively inhibits IKK-ε with an IC50 value of 40 nM and is essentially inactive at IKK-α and IKK-β.1
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Bamborough, P., Christopher, J.A., Cutler, G.J., et al. 5-(1H-benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-e kinase. Bioorg Med Chem Lett166236-6240(2006).
Bamborough, P., Christopher, J.A., Cutler, G.J., et al. 5-(1H-benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-e kinase. Bioorg Med Chem Lett166236-6240(2006).
CAY10576 is available in the following screening
library: