| CAS |
No.182498-32-4 |
| 英文名称 |
SB-225002 |
| 别名 |
1-(2-溴苯基)-3-(2-羟基-4-硝基苯基)脲 |
| 分子式 |
C13H10BrN3O4 |
| 分子量 |
352.14 |
| 溶解性 |
Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
| 纯度 |
≥98% |
| 外观(性状) |
White to yellow Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 |
冷藏运输 |
| MDL |
MFCD00078305 |
| SMILES |
O=C(NC1=CC=C([N+]([O-])=O)C=C1O)NC2=CC=CC=C2Br |
| 靶点 |
CXCR |
| 通路 |
Immunology & Inflammation;GPCR & G Protein |
| 背景说明 |
SB-225002是一种有效的选择性 CXCR2 非肽拮抗剂。 |
| 生物活性 |
SB225002 是一种有效的选择性 CXCR2 拮抗剂，IC50 为 22 nM。[1-5] |
| In Vitro |
SB225002(SB 225002)是125 I-IL-8与CXCR2结合的拮抗剂，IC 50 = 22 nM。 SB225002显示出比CXCR1和其他四种测试的7-TMR高150倍的选择性。 SB225002是一种有效的兔CXCR2拮抗剂，可抑制兔PMN趋化性，以响应人IL-8或GROα的最佳浓度(IC50值分别为30和70 nM。在这些细胞中(PMN，HL60，CXCR1-RBL-2H3)SB225002对IL-8和GROα介导的钙动员产生浓度依赖性抑制，IC50值分别为8和10 nM。在稳定转染CXCR2的3ASASE细胞中，SB 225002剂量依赖性地抑制两者诱导的钙动员。 GROα和IL-8，IC50值分别为20和40 nM [1]。用SB225002处理的WHCO1细胞表现出40％的细胞增殖减少。用400 nM SB225002(SB 225002)阻断WHCO1细胞中的CXCR2信号传导显著降低细胞增殖约40％至50％[2]。 |
| In Vivo |
SB225002(SB 225002)选择性地阻断兔中IL-8诱导的中性粒细胞边缘化[1]。使用选择性拮抗剂SB225002(2mg / kg)或中和CXCR2抗血清阻断CXCR2。在正常饮食中，CXCR2拮抗剂SB225002降低西方饮食和野生型小鼠ApoE - / - 小鼠缺血半球的中性粒细胞计数[3]。 SB225002显著减弱小胶质细胞激活和BBB损伤，增加髓鞘形成，并减少LPS致敏HI后白质中的星形胶质细胞增生[4]。 |
| 细胞实验 |
Three esophageal squamous cell carcinoma cell lines WHCO1，WHCO5，and WHCO6 originally established from surgical biopsies of primary esophageal squamous cell carcinomas are cultured in DMEM containing 10% FCS at 37°C in a humidified atmosphere of 5% CO2. MTT assays are carried out using the Cell Proliferation kit. Briefly，1.5×103 cells are plated in 96-well plates in a final volume of 180 μL DMEM per well. SB 225002(400 nM)is added to cells and 0.001% DMSO(solvent)is added as a control. After the indicated incubation period，18 μL of the MTT labeling reagent(final concentration 0.5 mg/mL)is added to each well and incubated for 4 hours in a humidified atmosphere. One hundred eighty microliters of the solubilization solution are added to each well and the plates are left overnight at 37°C. The spectrophotometric absorbance of samples is measured at 595 nm using a microtiter plate reader[2]. |
| 动物实验 |
Mice[3] |
| 激酶实验 |
CHO-CXCR1 and CHO-CXCR2 membranes are prepared. Assays are performed in 96-well microtiter plates where the reaction mixture contained 1.0 μg/mL membrane protein in 20 mM Bis-Tris-propane，pH 8.0，with 1.2 mM MgSO4，0.1 mM EDTA，25 mM NaCl，and 0.03% CHAPS and SB 225002(10 mM stock in Me2SO)added at the indicated concentrations，the final Me2SO concentration is <1% under standard binding conditions. Binding is initiated by addition of 0.25 nM 125I-IL-8(2，200 Ci/mmol). After 1-h incubation at room temperature the plate is harvested using a Tomtec 96-well harvester onto a glass fiber filtermat blocked with 1% polyethyleneimine，0.5% BSA and washed three times with 25 mM NaCl，10 mM Tris HCl，1 mM MgSO4，0.5 mMEDTA，0.03% CHAPS，pH 7.4. The filter is dried，sealed in a sample bag containing 10 mL of Wallac 205 Betaplate liquid scintillation fluid，and counted with a Wallac 1205 Betaplate liquid scintillation counter[1]. |
| 数据来源文献 |
[1]. White JR， et al. Identification of a potent， selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration. J Biol Chem. 1998 Apr 24;273(17):10095-8.
[2]. Wang B， et al. A growth-related oncogene/CXC chemokine receptor 2 autocrine loop contributes to cellular proliferation in esophageal cancer. Cancer Res. 2006 Mar 15;66(6):3071-7.
[3]. Herz J， et al. Role of Neutrophils in Exacerbation of Brain Injury After Focal Cerebral Ischemia in Hyperlipidemic Mice. Stroke. 2015 Oct;46(10):2916-25.
[4]. Wang LY， et al. CXCL5 signaling is a shared pathway of neuroinflammation and blood-brain barrier injury contributing to white matter injury in the immature brain. J Neuroinflammation. 2016 Jan 6;13:6.
[5]. Shi ZR， et al. Decrease of galectin-3 in keratinocytes: A potential diagnostic marker and a critical contributor to the pathogenesis of psoriasis. J Autoimmun. 2018 May;89:30-40. |
| 规格 |
5mg 10mg 25mg 50mg 100mg |
| 单位 |
瓶 |
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