| 名稱 | SB225002 |
| 描述 | SB225002 is a potent and selective CXCR2 antagonist inhibiting interleukin IL-8 binding to CXCR2. |
| 細(xì)胞實驗 | 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 I. Briefly, 1.5 × 103 cells are plated in 96-well plates in a final volume of 180 μL DMEM per well. SB 225002 (antagonist of CXCR2, 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 were left overnight at 37°C. The spectrophotometric absorbance of samples is measured at 595 nm using a microtiter plate reader.(Only for Reference) |
| 激酶實驗 | Radioligand Binding Experiments: Assays are performed in 96-well microtiter plates where the reaction mixture contains 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 mM EDTA, 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. |
| 體外活性 | SB225002表現(xiàn)出長效的鎮(zhèn)痛效果,并減少小鼠模型中TNBS誘導(dǎo)的結(jié)腸炎.在兔子中,SB225002選擇性阻斷IL-8誘導(dǎo)的嗜中性粒細(xì)胞的邊緣化.在小鼠肝內(nèi)膽管細(xì)胞癌模型中,1 mg/kg i.p. SB225002抑制皮下移植腫瘤的生長. |
| 體內(nèi)活性 | SB225002顯示了作為微管抑制劑的抗腫瘤活性。SB225002大大降低了磷酸化ERK1/2的水平,并降低了WHCO1細(xì)胞的細(xì)胞增殖。SB225002在體外實驗中,抑制GROα刺激的鈣動員,并有效地抑制由IL-8和GROα誘導(dǎo)的人和兔嗜中性粒細(xì)胞趨化性。 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 55 mg/mL (156.19 mM)
Ethanol : 3 mg/mL (8.51 mM), Heating is recommended.
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| 關(guān)鍵字 | SB-225002 | CXC chemokine receptors | CXCR | Inhibitor | inhibit | SB225002 | SB 225002 |
| 相關(guān)產(chǎn)品 | Nicotinamide N-oxide | Plerixafor octahydrochloride | Plerixafor | rac-NBI-74330 | LIT927 | CXCR2-IN-1 | SX-682 | Artemotil | Reparixin | AZD8309 | CXCL-CXCR1/2-IN-1 | Delmetacin |
| 相關(guān)庫 | 抑制劑庫 | 腫瘤免疫治療小分子化合物庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 細(xì)胞因子抑制劑庫 | ReFRAME 相關(guān)化合物庫 | 高選擇性抑制劑庫 | NO PAINS 化合物庫 | GPCR靶點分子庫 | 膜蛋白靶向化合物庫 |