BAY 11-7082, a potential anti-inflammatory agent, is an irreversible inhibitor of IKK α and phosphorylation of cytokine-inducible IκBα (nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor-α, NFKBIA; IC50=10 μM). In intact HUVECs, it inhibits TNFα-induced phosphorylation and degradation of IκBa (NFKBIA) without affecting constitutive phosphorylation. Inhibition of ιBα phosphorylation and degradation results in the inactivation of NFκB and thereby inhibits the expression of endothelial-leukocyte adhesion molecules: E-selectin, VCAM-1 and ICAM-11. BAY 11-7082 has also demonstrated stimulation of the stress-activated protein kinases, p38 and JNK-1. |