Cat. No. 2725
Chemical Name: N-(2-Bromophenyl)-N'-(2-hydroxy-4-ni
Biological ActivityPotent and selective CXCR2 chemokine receptor antagonist (IC50 = 22 nM) that displays > 150-fold selectivity over CXCR1 receptors. Causes inhibition of IL-8 and GROα-mediated calcium mobilization in HL60 cells (IC50 values are 8 and 10 nM respectively). Prevents IL-8-induced neutrophil chemotaxis in vitro and sequestration in vivo. Inhibits HIV replication in lymphocytes and macrophages.
Licensing InformationSold for research purposes under agreement from GlaxoSmithKline
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Catusse et al (2003) Characterization of the molecular interactions of interleukin-8 (CXCL8), growth related oncogen a (CXCL1) and a non-peptide antagonist (SB 225002) with the human CXCR2. Biochem.Pharmacol. 65 813. PMID: 12628493.
Lane et al (2001) Interleukin-8 stimulates human immunodeficiency virus type 1 replication and is a potential new target for antiretroviral therapy. J.Virol. 75 8195. PMID: 11483765.
White et al (1998) Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration. J.Biol.Chem. 273 10095. PMID: 9553055.
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Citations are publications that use Tocris products. Selected citations for SB 225002 include:
Devapatla et al (2015) CXCR2 Inhibition Combined with Sorafenib Improved Antitumor and Antiangiogenic Response in Preclinical Models of Ovarian Cancer. Stem Cells Transl Med 10 e0139237. PMID: 26414070.
Grabner et al (2015) Disruption of STAT3 signalling promotes KRAS-induced lung tumorigenesis. PLoS One 6 6285. PMID: 25734337.
Lourenco et al (2015) Macrophage migration inhibitory factor-CXCR4 is the dominant chemotactic axis in human mesenchymal stem cell recruitment to tumors. J Immunol 194 3463. PMID: 25712213.
Yuen et al (2012) Angiogenic dysfunction in bone marrow-derived early outgrowth cells from diabetic animals is attenuated by SIRT1 activation. J Clin Invest 1 921. PMID: 23283553.
Jang et al (2011) CXCL1 and its receptor, CXCR2, mediate murine sickle cell vaso-occlusion during hemolytic transfusion reactions. Sci Rep 121 1397. PMID: 21383500.
Toh et al (2011) Mesenchymal transition and dissemination of cancer cells is driven by myeloid-derived suppressor cells infiltrating the primary tumor. PLoS Biol 9 e1001162. PMID: 21980263.
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Keywords: SB 225002, supplier, Potent, selective, CXCR2, antagonists, Chemokine, Receptors, SB225002, GlaxoSmithKline, GSK, Tocris Bioscience, Chemokine CXC Receptor Antagonist products
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