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.

Cell permeable: yes

Primary Target
TNF-α-inducible phosphorylation of IκBα

Product does not compete with ATP.

Reversible: no

Packaged under inert gas

Supplied as a 100 mM (10 mg/483 µl) solution of BAY 11-7082 (Cat. No. 196870) in DMSO.

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.

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

Toxicity: Irritant (B)