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BAY-11-7082

Cayman Chemical Item Number 10010266

(CAS 19542-67-7)

BAY-11-7082 (CAS 19542-67-7)

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Description

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

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).

Formal Name 3-​[(4-​methylphenyl)sulfonyl]-​(2E)-​propenenitrile
CAS Number 19542-67-7
Molecular Formula C10H9NO2S
Formula Weight 207.3
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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N#C/C=C/S(=O)​(=O)​c1ccc(C)​cc1

Background Reading

Karin, M. The beginning of the end: IκB kinase (IKK) and NF-κB activation. J Biol Chem 274(39) 27339-27342 (1999).

Pahl, H.L. Activators and target genes of Rel/NF-κB transcription factors. Oncogene 18 6853-6866 (1999).

Gilmore, T.D. The Rel/NF-κB signal transduction pathway: Introduction. Oncogene 18 6842-6844 (1999).

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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Size Price Quantity Subtotal
5 mg $39.00 $0.00
10 mg $74.00 $0.00
25 mg $176.00 $0.00
50 mg $312.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-05-25. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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