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KI3285SB-225002QuoteQuote

Chemical Characteristic

Product NameSB-225002
CAS No.182498-32-4
Molecular Weight 352.14
FormulaC13H10BrN3O4
Chemical Structure

Biological activities

SB-225002 is a potent, selective non-peptide CXCR2 antagonist. SB-225002 inhibits 125I-IL-8 binding to CXCR2 with an IC50 of 22 nM. However, SB 225002 displays >150-fold selectivity over CXCR1. In 3ASubE cells stably transfected with CXCR2 in vitro, SB 225002 inhibits calcium mobilization induced by both GROα and IL-8 in a does-dependent manner, with IC50 values of 20 and 40 nM, respectively. In vitro, SB 225002 significantly inhibits human and rabbit neutrophil chemotaxis induced by both GROα and IL-8.[1] SB 225002 potently inhibits the proliferation of WHCO1 cells in vitro.[2] SB-225002 also inhibits HIV-1 replication in both T lymphocytes and macrophages in vitro.[3] In vivo, SB 225002 selectively blocks neutrophil margination induced by IL-8 in rabbits.[1] In vivo, curative treatment with SB 225002 also significantly ameliorates acute 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis in mice, along with the reduction of neutrophil influx, myeloperoxidase (MPO) activity, IL-1β, MIP-2, and keratinocyte-derived chemokine (KC) levels and the decreased expression of vascular endothelial growth factor (VEGF), inducible NO synthase (iNOS), and cyclooxygenase-2 (Cox-2) proteins into the colon tissue.[4]

Protocols

In vitro: SB-225002 is dissolved in dimethyl sulfoxide (DMSO).[5]

References

[1] White JR, et al. Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration. J Biol Chem. 1998, 273(17): 10095-10098.
[2] Wang B, et al. A growth-related oncogene/CXC chemokine receptor 2 autocrine loop contributes to cellular proliferation in esophageal cancer. Cancer Res. 2006, 66(6): 3071-3077.
[3] Lane BR, et al. Interleukin-8 stimulates human immunodeficiency virus type 1 replication and is a potential new target for antiretroviral therapy. J Virol. 2001, 75(17): 8195-8202.
[4] Bento AF, et al. The selective nonpeptide CXCR2 antagonist SB225002 ameliorates acute experimental colitis in mice. J Leukoc Biol. 2008, 84(4): 1213-1221.
[5] Steude J, et al. Interleukin-1-stimulated secretion of interleukin-8 and growth-related oncogene-alpha demonstrates greatly enhanced keratinocyte growth in human raft cultured epidermis. J Invest Dermatol. 2002, 119(6): 1254-1260.

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