SB 225002

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. SB 225002 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, SB 225002 reduces neutrophil influx, the production of inflammatory mediators, and tissue damage in TNBS-induced colitis in mice.²

WARNING This product is not for human or veterinary use.

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. The Journal of Biological Chemisty 273(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. Biol. 84(4), 1213-1221 (2008).