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Submit ReviewSB 225002
说明： Potent and selective CXCR2 antagonist
化学名： N-(2-Bromophenyl)-N'-(2-hydroxy-4-nitrophenyl)urea
纯度： ≥99% (HPLC)
生物活性 for SB 225002
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.
许可信息
Sold for research purposes under agreement from GlaxoSmithKline
化合物库 for SB 225002
SB 225002 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
技术数据 for SB 225002
| 分子量 | 352.14 |
| 公式 | C13H10BrN3O4 |
| 储存 | Store at RT |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for SB 225002
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 35.21 | 100 | |
| ethanol | 17.61 | 50 |
制备储备液 for SB 225002
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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 |
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产品说明书 for SB 225002
参考文献 for SB 225002
参考文献是支持产品生物活性的出版物。
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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关键词: SB 225002, SB 225002 supplier, Potent, selective, CXCR2, antagonists, Chemokine, Receptors, SB225002, GlaxoSmithKline, GSK, CXC, 2725, Tocris Bioscience
12 篇 SB 225002 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SB 225002 的部分引用包括：
Saika (2018) Chemokine CXCL1 is responsible for cocaine-induced reward in mice. NeurosciPharm Reports 38 145 PMID: 30175527
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
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
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
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
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
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
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
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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SB 225002 的评论
平均评分: 4 (Based on 1 Review.)
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Used for Migration assays.
By
Anonymous on 07/01/2020
分析类型： In Vitro
种属： Human
细胞系/组织： A549 or MDAMB231
Receptor antagonists (SB225002: for CXCR2, AMD3465: for CXCR4, RS504393: for CCR2 and Maraviroc: for CCR5) at 10 μM
We ordered this product, combining with another inhibitor, to confirm the migration.To confirm that tested product induces migration, we also screen all MAPK inhibitors and MIF receptor antagonists
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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