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10010266 BAY-11-7082
(CAS 19542-67-7)
BAY-11-7082 Workbook Links
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The transcription factor NF-κB plays a key role in regulating over 150 target genes including the expression of inflammatory cytokines, chemokines, immunoreceptors, and cell adhesion molecules.1 In the cytoplasm, inactive NF-κB complexes are bound to an inhibitor IκB.2 However in response to certain stimuli, IκB is phosphorylated, ubiquitinated, and degraded, enabling the translocation of NF-κB to the nucleus.3 BAY-11-7082 selectively and irreversibly inhibits NF-κB activation by blocking TNF-α-induced phosphorylation of IκB-α without affecting constitutive IκB-α phosphorylation.4 This compound inhibits the TNF-α-induced surface expression of adhesion molecules ICAM-1, VCAM-1, and E-selectin in human endothelial cells with IC50 values of 5-10 µM.4
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1
Pahl, H.L. Activators and target genes of Rel/NF-κB transcription factors. Oncogene 18 6853-6866 (1999).
2
Gilmore, T.D. The Rel/NF-κB signal transduction pathway: Introduction. Oncogene 18 6842-6844 (1999).
3
Karin, M. The beginning of the end: IκB kinase (IKK) and NF-κB activation. J Biol Chem 274(39) 27339-27342 (1999).
4
Pierce, J.W., Schoenleber, R., Jesmok, G., et al. Novel inhibitors of cytokine-induced IkBa phosphorylation and endothelial cell adhesion molecule expression show anti-inflammatory effects in vivo. J Biol Chem 272(34) 21096-21103 (1997).
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Pricing updated 2010-03-18.
Prices are subject to change without notice.
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Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.
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