Biological Activity
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.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Compound Libraries
SB 225002 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 352.14 |
| Formula | C13H10BrN3O4 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 182498-32-4 |
| PubChem ID | 3854666 |
| InChI Key | MQBZVUNNWUIPMK-UHFFFAOYSA-N |
| Smiles | OC1=CC(=CC=C1NC(=O)NC1=CC=CC=C1Br)[N+]([O-])=O |
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.
Solubility Data
| DMSO | 35.21 | 100 |
| ethanol | 17.61 | 50 |
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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 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 |
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Certificate of Analysis / Product Datasheet Safety Datasheet Select another language: English German French Spanish View SDSReferences
References are publications that support the products\' biological activity.
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
Keywords: SB 225002, supplier, Potent, selective, CXCR2, antagonists, Chemokine, Receptors, SB225002, GlaxoSmithKline, GSK, Chemokine, CXC, Receptors, Chemokine, CXC, Receptors, Tocris Bioscience
