CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and growth related oncogene α (Gro-α; CXCL1). IL-8 and Gro-α are pro-inflammatory CXC chemokines that act as chemoattractants, especially for neutrophils, and promote angiogenesis. SB225002 is a selective non-peptide inhibitor of CXCR2, inhibiting IL-8 binding to CXCR2 with an IC50 value of 22 nM.1 SB225002 inhibits neutrophil chemotaxis in response to IL-8 in vitro (IC50 = 20 nM) and blocks neutrophil margination induced by IL-8 in vivo (IC50 = 30 nM).1 Similarly, SB225002 reduces neutrophil influx, the production of inflammatory mediators, and tissue damage in TNBS-induced colitis in mice.2
1
White, J.R., Lee, J.M., Young, P.R., et al. Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration. J Biol Chem273(17)10095-10098(1998).
2
Bento, A.F., Leite, D.F.P., Claudino, R.F., et al. The selective nonpeptide CXCR2 antagonist SB225002 ameliorates acute experimental colitis in mice. J Leukoc Biol841213-1221(2008).