Home / Chemokine Receptor Antagonists / SB 225002

SB 225002

Catalog #: 2725
12 Citations 1 Review Datasheet / COA / SDS
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SB 225002 | CAS No. 182498-32-4 | Chemokine Receptor Antagonists
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Description: Potent and selective CXCR2 antagonist

Chemical Name: N-(2-Bromophenyl)-N'-(2-hydroxy-4-nitrophenyl)urea

Purity: ≥99%

Product Details
Citations (12)
Reviews (1)
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

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

M.Wt:
352.14
Formula:
C13H10BrN3O4
Solubility:
Soluble to 100 mM in DMSO and to 50 mM in ethanol
Purity:
≥99%
Storage:
Store at RT
CAS No:
182498-32-4

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

Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline

Background References

  1. Macrophage migration inhibitory factor-CXCR4 is the dominant chemotactic axis in human mesenchymal stem cell recruitment to tumors.
    Lourenco S, Teixeira V, Kalber T, Jose R, Floto R, Janes S
    J Immunol, 2015;194(7):3463-74.
  2. CXCR2 and its related ligands play a novel role in supporting the pluripotency and proliferation of human pluripotent stem cells.
    Jung J, Lee S, Kim J, Lee S, Sung H, An J, Park Y, Kim B
    Stem Cells Dev, 2015;24(8):948-61.
  3. G protein-coupled receptor kinase 6 deficiency promotes angiogenesis, tumor progression, and metastasis.
    Raghuwanshi S, Smith N, Rivers E, Thomas A, Sutton N, Hu Y, Mukhopadhyay S, Chen X, Leung T, Richardson R
    J Immunol, 2013;190(10):5329-36.
  4. 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
  5. 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
  6. 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
  7. Complement receptor C3aR1 controls neutrophil mobilization following spinal cord injury through physiological antagonism of CXCR2
    FH Brennan, T Jogia, ER Gillespie, LV Blomster, XX Li, B Nowlan, GM Williams, E Jacobson, GW Osborne, FA Meunier, SM Taylor, KE Campbell, KP MacDonald, JP Levesque, TM Woodruff, MJ Ruitenberg
    JCI Insight, 2019;4(9):.

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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

  1. 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
  2. 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
  3. Chemokine CXCL1 is responsible for cocaine-induced reward in mice.
    Authors: Saika
    NeurosciPharm Reports  2018;38(3):145
  4. 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
  5. Disruption of STAT3 signalling promotes KRAS-induced lung tumorigenesis.
    Authors: Grabner Et al.
    PLoS One  2015;6:6285
  6. 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
  7. 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
  8. 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
  9. 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
  10. 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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SB 225002
By Anonymous on 08/22/2016
Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.