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| | SB 225002 Basic information |
| | SB 225002 Chemical Properties |
| Boiling point | 401.6±45.0 °C(Predicted) | | density | 1.793±0.06 g/cm3(Predicted) | | storage temp. | room temp | | solubility | Soluble to 100mM in DMSO and to 50mM in ethanol | | form | Yellow solid | | pka | 5.29±0.10(Predicted) | | color | white to beige | | Sensitive | Moisture Sensitive | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. | | InChIKey | MQBZVUNNWUIPMK-UHFFFAOYSA-N | | CAS DataBase Reference | 182498-32-4 |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26 | | WGK Germany | 3 | | HS Code | 2921490090 |
| | SB 225002 Usage And Synthesis |
| Description | CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and growth related oncogene α (Gro-α; CXCL1). IL-8 and Gro-α are pro-inflammatory CXC chemokines that act as chemoattractants, especially for neutrophils, and promote angiogenesis. SB 225002 is a selective non-peptide inhibitor of CXCR2, inhibiting IL-8 binding to CXCR2 with an IC50 value of 22 nM. SB225002 inhibits neutrophil chemotaxis in response to IL-8 in vitro (IC50 = 20 nM) and blocks neutrophil margination induced by IL-8 in vivo (IC50 = 30 nM). Similarly, SB 225002 reduces neutrophil influx, the production of inflammatory mediators, and tissue damage in TNBS-induced colitis in mice. | | Uses | SB 225002 is a potent and selective CXCR2 antagonist with the ability to inhibit interleukin IL-8 binding to CXCR2. | | Definition | ChEBI: 1-(2-bromophenyl)-3-(2-hydroxy-4-nitrophenyl)urea is a nitrophenol. | | Biological Activity | Potent and selective CXCR2 chemokine receptor antagonist (IC 50 = 22 nM) that displays > 150-fold selectivity over CXCR1 receptors. Causes inhibition of IL-8 and GRO α -mediated calcium mobilization in HL60 cells (IC 50 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. | | Biochem/physiol Actions | SB-225002 is a potent nonpeptide inhibitor of chemokine receptor CXCR2 with an IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2 and > 150-fold selectivity over CXCR1 receptors. CXCR2 binds many different immune cell chemoattractants. SB-225002 is crucial for cancer progression and is involved in inflammatory diseases like COPD, rheumatoid arthritis, and ulcerative colitis. | | storage | Store at RT | | References | 1) 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
2) Du et al. (2013) SB225002 Promotes Mitotic Catastrophe in Chemo-Sensitive and -Resistant Ovarian Cancer Cells Independent of p53 Status In Vitro; PLoS One. 8 e54572
3) Shen et al. (2013), Interleukin-8 prevents oxidative stress-induced human endothelial cell senescence via telomerase activation; Int. Immunopharmacol. 16 261
4) 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
5) Wu et al. (2015), CXCR2 is essential for cerebral endothelial activation and leukocyte recruitment during neuroinflammation; J. Neuroinflammation 12 98 |
| | SB 225002 Preparation Products And Raw materials |
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