General Description
Potential anti-inflammatory agent. Selectively and irreversibly inhibits the TNFα-inducible phosphorylation of IκB-α (IC
50 = 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 (IC
50 ~10 μM). Also reversibly increased the activity of p38 kinase and JNK-1 and stimulated tyrosine phosphorylation of a 130-140 kDa protein.
