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Description

Potential anti-inflammatory agent. Selectively and irreversibly inhibits the TNFalpha-inducible phosphorylation of IkappaB-alpha (IC50 = 10 µ,M) without affecting the constitutive IkappaB-alpha phosphorylation. Decreases nuclear translocation of NFkappaB and inhibits TNFalpha-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 µ,M). Also reversibly increased the activity of p38 kinase and JNK-1 and stimulated tyrosine phosphorylation of a 130-140 kDa protein.