IKK-3 Inhibitor

"目录号: HY-14682

NF-κB-

IKK-3抑制剂是IKK-ε选择性抑制剂，IC50为40 nM，对IKK-α和 IKK-β无活性。

IKK

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生物活性

Description

IKK-3 Inhibitor is a potent, selective, inhibitor of IKK-epsilon kinase with IC50 of 40 nM; inactive at IKK-α and IKK-β.IC50 value: 40 nMTarget: IKK-epsilonThe 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. It 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.

References

[1].Bamborough P, et al. 5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-epsilon kinase. Bioorg Med Chem Lett. 2006 Dec 15;16(24):6236-40.