Biochem/physiol Actions

Reversible: no

Target IC₅₀: 10 µM inhibiting TNF-α-inducible phosphorylation of IκBα

Primary TargetTNF-α-inducible phosphorylation of IκBα

Cell permeable: yes

General description

Potential anti-inflammatory agent that selectively and irreversibly inhibits the TNF-α-inducible phosphorylation of IκBα (IC₅₀ = 10 µM), resulting in a decreased expression of NF-κB and of adhesion molecules. Does not affect constitutive IκBα autophosphorylation. Inhibits TNF-α-induced surface expression of the endothelial-leukocyte cell adhesion molecules E-selectin, VCAM-1, and ICAM-1. A 100 mM (10 mg/483 µl) solution of BAY 11-7082 (Cat. No. 196871) in DMSO is also available is also available.

Potential anti-inflammatory agent. Selectively and irreversibly inhibits the TNFα-inducible phosphorylation of IκB-α (IC₅₀ = 10 µM) without affecting the constitutive IκB-α phosphorylation. Decreases nuclear translocation of NFκB and inhibits TNFα-induced surface expression of the endothelial-leukocyte cell adhesion molecules E-selectin, VCAM-1, and ICAM-1. E-selectin inhibition was shown to be irreversible (IC₅₀ ~10 µM). Also reversibly increased the activity of p38 kinase and JNK-1 and stimulated tyrosine phosphorylation of a 130-140 kDa protein.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Kamthong PJ. and Wu, M-C. 2001. Biochem. J. 356.Izban, K.F., et al. 2000. Hum. Pathol.31, 1482.Pierce, J.W., et al. 1997. J. Biol. Chem. 272, 21096.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)