A 205804 is a selective E-selectin and ICAM-1 inhibitor over VCAM-1. When tested with primary HUVECs cells, A-205804 treatment reduced cell migration ability by inhibiting the expression of E-selectin and ICAM-1. In human vascular endothelial cells using whole-cell high-throughput assay, it was shown that A 205804 exhibited potent and selective inhibition to E-selectin and ICAM-1 with low concentrations. Further, it was revealed that A 205804 inhibited E-selectin and ICAM-1 expressions by translocating to cell nucleus and noncovalently associated with macromolecules of molecular weight greater than 650 kDa when tested with human umbilical vein endothelial cells (HUVECs).