A 205804

Description

A-205804 is a potent inhibitor of E-selectin and ICAM-1 expression in human vascular endothelial cells stimulated with TNF-α (IC₅₀s = 20 and 25 nM, respectively). It does not block expression of VCAM-1 (IC₅₀ > 1,000 nM).

Uses

4-[(4-Methylphenyl)thio]thieno[2,3-c]pyridine-2-carboxamide is a reagent used in the preparation of selective inhibitors of cell adhesion molecule expression in human endothelial cells.

Definition

ChEBI: 4-[(4-methylphenyl)thio]-2-thieno[2,3-c]pyridinecarboxamide is an aryl sulfide.

Biological Activity

Selective inhibitor of E-selectin and ICAM-1 expression (IC 50 values are 20, 25 and > 1000 nM for TNF- α -induced E-selectin, ICAM-1 and VCAM-1 expression respectively). Effective inhibitor of cell-cell adhesion in an in vitro flow experiment.

storage

Store at +4°C

References

[1]. stewart, a.o., et al., discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. selective inhibition of icam-1 and e-selectin expression. j med chem, 2001. 44(6): p. 988-1002.
[2]. chang, c.z., et al., valproic acid attenuates intercellular adhesion molecule-1 and e-selectin through a chemokine ligand 5 dependent mechanism and subarachnoid hemorrhage induced vasospasm in a rat model. j inflamm (lond), 2015. 12: p. 27.
[3]. zhu, g.d., et al., selective inhibition of icam-1 and e-selectin expression in human endothelial cells. 2. aryl modifications of 4-(aryloxy)thieno[2,3-c]pyridines with fine-tuning at c-2 carbamides. j med chem, 2001. 44(21): p. 3469-87.
[4]. zhu, g.d., et al., synthesis and mode of action of (125)i- and (3)h-labeled thieno[2,3-c]pyridine antagonists of cell adhesion molecule expression. j org chem, 2002. 67(3): p. 943-8.