10011249  CAY10576

(CAS 862812-98-4)

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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
1  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. Biooganic & Medicinal Chemistry Letters 16 6236-6240 (2006).


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Pricing updated 2010-03-19.
Prices are subject to change without notice.

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