A-205804 selectively inhibits the surface expression of the cell adhesion molecules ICAM-1 and E-selectin in human endothelial cells. A-205804 inhibites the IL-1β-induced expression of E-selectin (IC50 = 20 nM) and ICAM-1 (IC50 = 10 nM) with essentially the same level of potency as that for TNFα-induced expression. For reasons which are unclear, the ability of A-205804 to inhibit PMA-induced E-selectin expression is significantly reduced (IC50 > 1000 nM), but A-205804 is a potent inhibitor of ICAM-1 expression (IC50 = 40 nM) using this protein-kinase C-activating agent.