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Purity: ≥98%
SB225002 (SB 225002; SB-225002) is a novel, potent, and selective non-peptide antagonist of chemokine receptor CXCR2 with potential anti-inflammatory activity. It blocks the binding of interleukin 125I-IL-8 to CXCR2 and inhibits CXCR2 with an IC50 of 22 nM as well. More than 150 times as selective as CXCR1 and the other four 7-TMRs tested was demonstrated by SB 225002. The chemotaxis of human and rabbit neutrophils induced by IL-8 and GROalpha was potently inhibited in vitro by SB 225002. Rabbits' neutrophil margination caused by IL-8 was specifically inhibited in vivo by SB 225002. According to the current research, CXCR2 is in charge of IL-8-induced neutrophil chemotaxis and margination. It has also been reported that SB225002 functions as a mitotic inhibitor, independent of p53 status, to induce mitotic catastrophe in chemo-sensitive and -resistant ovarian cancer cells in vitro. By different means, SB225002 causes ovarian cancer (OVCA) cells with and without p53 to undergo apoptosis. This selective antagonist will be an effective tool in defining CXCR2's function in inflammatory diseases where neutrophils are important players.
Targets |
125I-IL-8-CXCR2 ( IC50 = 22 nM )
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
There are ready membranes for CHO-CXCR1 and CHO-CXCR2. The experiments are carried out in 96-well microtiter plates with 1.0 μg/mL membrane protein in 20 mM Bis-Tris-propane, pH 8.0, and 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. Under standard binding conditions, the final Me2SO concentration is less than 1%. When 0.25 nM 125I-IL-8 (2,200 Ci/mmol) is added, binding is started. The plate is harvested onto a glass fiber filtermat blocked with 1% polyethyleneimine and 0.5% BSA after a one-hour incubation period at room temperature. The plate is then cleaned three times using 25 mM NaCl, 10 mM Tris•HCl, 1 mM MgSO4, 0.5 mMEDTA, 0.03% CHAPS, and pH 7.4. The filter is sealed in a sample bag with 10 mL of Wallac 205 Betaplate liquid scintillation fluid after it has dried, and a Wallac 1205 Betaplate liquid scintillation counter is used to count the results.
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Cell Assay |
Three esophageal squamous cell carcinoma cell lines—WHCO1, WHCO5, and WHCO6—are cultured in DMEM containing 10% FCS at 37°C in a humidified atmosphere with 5% CO2. These cell lines were initially established from surgical biopsies of primary esophageal squamous cell carcinomas. To perform MTT assays, use the Cell Proliferation kit. In 96-well plates, 1.5×103 cells are plated with a final volume of 180 μL DMEM per well. Cells are treated with 400 nM of SB 225002, and as a control, 0.001% DMSO (solvent) is added. Following the specified incubation time, each well receives 18 μL of the MTT labeling reagent (final concentration 0.5 mg/mL), which is then incubated for 4 hours in a humidified environment. The solubilization solution is poured into each well in a volume of 180,000 microliters, and the plates are then left at 37°C overnight. A microtiter plate reader is used to measure the samples' spectrophotometric absorbance at 595 nm.
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Animal Protocol |
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References |
Molecular Formula |
C13H10BRN3O4
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Molecular Weight |
352.14
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Exact Mass |
350.99
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Elemental Analysis |
C, 44.34; H, 2.86; Br, 22.69; N, 11.93; O, 18.17
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CAS # |
182498-32-4
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Appearance |
White solid powder
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SMILES |
C1=CC=C(C(=C1)NC(=O)NC2=C(C=C(C=C2)[N+](=O)[O-])O)Br
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InChi Key |
MQBZVUNNWUIPMK-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C13H10BrN3O4/c14-9-3-1-2-4-10(9)15-13(19)16-11-6-5-8(17(20)21)7-12(11)18/h1-7,18H,(H2,15,16,19)
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Chemical Name |
1-(2-bromophenyl)-3-(2-hydroxy-4-nitrophenyl)urea
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Synonyms |
SB225002; SB 225002; SB225002
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8398 mL | 14.1989 mL | 28.3978 mL | |
5 mM | 0.5680 mL | 2.8398 mL | 5.6796 mL | |
10 mM | 0.2840 mL | 1.4199 mL | 2.8398 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Competition binding of125I-IL-8, [3H]FMLP, [3H]LTB4, [3H]LTD4, or125I-C5a by SB 225002 to appropriate membranes expressing either cloned or primary receptors.J Biol Chem.1998 Apr 24;273(17):10095-8. th> |
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Effect of SB 225002 on IL-8-, GROα-, or C5a-induced human neutrophil chemotaxis.J Biol Chem.1998 Apr 24;273(17):10095-8. td> |
Effect of SB 225002 on IL-8- and fMLP-induced neutrophil margination in rabbits.J Biol Chem.1998 Apr 24;273(17):10095-8. td> |