A benzothiophene-carboxamide is a potent inhibitor of IL-1beta induced VCAM-1 gene expression in human endothelial cells.

Vascular endothelial cells respond to cytokines such as IL-1β or TNF-α by undergoing a number of functional alterations. Among these alterations is the induction of cell surface adhesion molecules, including VCAM-1. In this report, we investigated the effects of a 3-alkoxybenzo[β]thiopene-2-carboximide (BZT) on the cytokine induction of VCAM-1 expression and activation of the transcription factor NF-κB in human endothelial cells. BZT blocked the IL-1β induced cell surface expression of VCAM-1 in human endothelial cells but did not prevent nuclear translocation of NF-κB. This study demonstrates that BZT is a potent inhibitor of VCAM-1 expression in human endothelial cells.