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Potent 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.
Sold for research purposes under agreement from GlaxoSmithKline
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 352.14. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.84 mL||14.2 mL||28.4 mL|
|5 mM||0.57 mL||2.84 mL||5.68 mL|
|10 mM||0.28 mL||1.42 mL||2.84 mL|
|50 mM||0.06 mL||0.28 mL||0.57 mL|
References are publications that support the biological activity of the product.
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
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
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
If you know of a relevant reference for SB 225002, please let us know.
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Keywords: SB 225002, SB 225002 supplier, Potent, selective, CXCR2, antagonists, Chemokine, Receptors, SB225002, GlaxoSmithKline, GSK, CXC, 2725, Tocris Bioscience
12 Citations for SB 225002
Citations are publications that use Tocris products. Selected citations for SB 225002 include:
Grabner et al (2015) Disruption of STAT3 signalling promotes KRAS-induced lung tumorigenesis. PLoS One 6 6285 PMID: 25734337
Devapatla et al (2015) CXCR2 Inhibition Combined with sora. Improved Antitumor and Antiangiogenic Response in Preclinical Models of Ovarian Cancer. Stem Cells Transl Med 10 e0139237 PMID: 26414070
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
Saika (2018) Chemokine CXCL1 is responsible for cocaine-induced reward in mice. NeurosciPharm Reports 38 145 PMID: 30175527
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
Karim et al (2019) Analogues of ERβ ligand chloroindazole exert immunomodulatory and remyelinating effects in a mouse model of multiple sclerosis. Sci Rep 9 503 PMID: 30679747
Chen et al (2019) Cancer-Derived VEGF-C Increases Chemokine Production in Lymphatic Endothelial Cells to Promote CXCR2-Dependent Cancer Invasion and MDSC Recruitment. Cancers (Basel) 11 PMID: 31390756
Jung et al (2016) CXCR2 Inhibition in Human Pluripotent Stem Cells Induces Predominant Differentiation to Mesoderm and Endoderm Through Repression of mTOR, β-Catenin, and hTERT Activities. Stem Cells Dev 25 1006 PMID: 27188501
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
Raccosta et al (2013) The oxysterol-CXCR2 axis plays a key role in the recruitment of tumor-promoting neutrophils. J Exp Med 210 1711 PMID: 23897983
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
Lavoie-Lamoureux et al (2010) IL-4 activates equine neutrophils and induces a mixed inflammatory cytokine expression profile with enhanced neutrophil chemotactic mediator release ex vivo. Am J Physiol Lung Cell Mol Physiol 299 L472 PMID: 20639353
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Reviews for SB 225002
Average Rating: 4 (Based on 1 Review.)
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