SB 225002
Chemical Name: N-(2-Bromophenyl)-N'-(2-hydroxy-4-nitrophenyl)urea
Purity: ≥99%
Biological Activity
SB 225002 is a 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.Technical Data
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.
Additional Information
Background References
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Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration.
White et al.
J.Biol.Chem., 1998;273:10095 -
Interleukin-8 stimulates human immunodeficiency virus type 1 replication and is a potential new target for antiretroviral therapy.
Lane et al.
J.Virol., 2001;75:8195 -
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.
Catusse et al.
Biochem.Pharmacol., 2003;65:813
Product Datasheets
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Citations for SB 225002
The citations listed below are publications that use Tocris products. Selected citations for SB 225002 include:
12 Citations: Showing 1 - 10
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Analogues of ERβ ligand chloroindazole exert immunomodulatory and remyelinating effects in a mouse model of multiple sclerosis.
Authors: Karim Et al.
Sci Rep 2019;9:503
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Cancer-Derived VEGF-C Increases Chemokine Production in Lymphatic Endothelial Cells to Promote CXCR2-Dependent Cancer Invasion and MDSC Recruitment.
Authors: Chen Et al.
Cancers (Basel) 2019;11
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Chemokine CXCL1 is responsible for cocaine-induced reward in mice.
Authors: Saika
NeurosciPharm Reports 2018;38(3):145
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CXCR2 Inhibition in Human Pluripotent Stem Cells Induces Predominant Differentiation to Mesoderm and Endoderm Through Repression of mTOR, β-Catenin, and hTERT Activities.
Authors: Jung Et al.
Stem Cells Dev 2016;25:1006
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Disruption of STAT3 signalling promotes KRAS-induced lung tumorigenesis.
Authors: Grabner Et al.
PLoS One 2015;6:6285
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Macrophage migration inhibitory factor-CXCR4 is the dominant chemotactic axis in human mesenchymal stem cell recruitment to tumors.
Authors: Lourenco Et al.
J Immunol 2015;194:3463
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CXCR2 Inhibition Combined with sora. Improved Antitumor and Antiangiogenic Response in Preclinical Models of Ovarian Cancer.
Authors: Devapatla Et al.
Stem Cells Transl Med 2015;10:e0139237
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The oxysterol-CXCR2 axis plays a key role in the recruitment of tumor-promoting neutrophils.
Authors: Raccosta Et al.
J Exp Med 2013;210:1711
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Angiogenic dysfunction in bone marrow-derived early outgrowth cells from diabetic animals is attenuated by SIRT1 activation.
Authors: Yuen Et al.
J Clin Invest 2012;1:921
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Mesenchymal transition and dissemination of cancer cells is driven by myeloid-derived suppressor cells infiltrating the primary tumor.
Authors: Toh Et al.
PLoS Biol 2011;9:e1001162
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CXCL1 and its receptor, CXCR2, mediate murine sickle cell vaso-occlusion during hemolytic transfusion reactions.
Authors: Jang Et al.
Sci Rep 2011;121:1397
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IL-4 activates equine neutrophils and induces a mixed inflammatory cytokine expression profile with enhanced neutrophil chemotactic mediator release ex vivo.
Authors: Lavoie-Lamoureux Et al.
Am J Physiol Lung Cell Mol Physiol 2010;299:L472
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