| Name | SB225002 |
| Description | SB225002 is a potent and selective CXCR2 antagonist inhibiting interleukin IL-8 binding to CXCR2. |
| Cell Research | 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) |
| Kinase Assay | 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. |
| In vitro | SB225002 demonstrates prolonged analgesic effects and reduces TNBS-induced colitis in mouse models. In rabbits, SB225002 selectively inhibits the margination of neutrophils induced by IL-8. Moreover, at a dosage of 1 mg/kg i.p., SB225002 suppresses the growth of subcutaneously transplanted tumors in a mouse model of intrahepatic cholangiocarcinoma. |
| In vivo | SB225002 demonstrates antitumor activity as a microtubule inhibitor. It significantly reduces the levels of phosphorylated ERK1/2 and decreases the proliferation of WHCO1 cells. In vitro, SB225002 inhibits calcium mobilization stimulated by GROα and effectively suppresses the chemotaxis of human and rabbit neutrophils induced by IL-8 and GROα. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (156.19 mM)
Ethanol : 3 mg/mL (8.51 mM), Heating is recommended.
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| Keywords | SB-225002 | CXC chemokine receptors | CXCR | Inhibitor | inhibit | SB225002 | SB 225002 |
| Inhibitors Related | AZD8309 | rac-NBI-74330 | Delmetacin | Tannic acid | Artemotil | CXCR2-IN-1 | LIT927 | Reparixin | Plerixafor octahydrochloride | Nicotinamide N-oxide | Plerixafor | CXCL-CXCR1/2-IN-1 |
| Related Compound Libraries | Highly Selective Inhibitor Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | NO PAINS Compound Library | Stem Cell Differentiation Compound Library | Immuno-Oncology Compound Library | Bioactive Compounds Library Max | GPCR Compound Library |
United States
