Molecular Weight(MW): 352.14
SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.
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The inhibitor SB225002 significantly decreased J82-, CXCL2- or MIF-mediated MDSC migration. The bars represent the s.e.m. of three experiments. *P<0.05.
Oncogene, 2017, 36(15):2095-2104. SB225002 purchased from Selleck.
(e, f) Administration of the selective CXCR2 antagonist SB225002 mitigated mechanical hyperalgesia and heat hyperalgesia in CCI rats. Antinociceptive effects of a single intrathecal (it.) injection of 20 µg SB225002 were observed at 1 h and disappeared at 2 h. Antinociceptive effects induced by a single injection of SB225002 at 40 µg were observed at 1 h and disappeared 6 h after injection. Injection of SB225002 (10 µg, i.t.) did not alter the PWT and PWL of CCI rats. N = 6 rats for each group, *p < .05, compared to NS group. PWL: paw withdraw latency; PWT: paw mechanical withdrawal thresholds.
Mol Pain, 2016.. SB225002 purchased from Selleck.
The irradiated Beas-2B cells were further co-cultured with U937 cells for 24 h after irradiation. In some experiments, Beas-2B cells were pretreated with 10 μM of U0126, SB203580, or necrostatin-1 for 1 h before irradiation, U937 cells were pretreated with 10 μM BAY 11-7082 1 h prior to cell co-culture, or 1 μg/ml anti-TNF-a antibody, 2 μg/ml anti-IL-8 antibody,40 nM SB225002 were added to the medium in the cell co-culture period. ***P < 0.001 compared with the non-irradiation control. #P < 0.05 ##P < 0.01 compared with cor-responding -irradiated cells.
Mutation Research, 2016, 789:1-8.. SB225002 purchased from Selleck.
Purity & Quality Control
Choose Selective CXCR Inhibitors
|Description||SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.|
In vitro, SB225002 inhibits GROα-stimulated calcium mobilization, and potently inhibits human and rabbit neutrophil chemotaxis induced by both IL-8 and GROalpha.  SB 225002 substantially reduces the levels of phosphorylated ERK1/2, and decreases cell proliferation in WHCO1 cells.  SB225002 also shows the antitumor activity as a microtubule inhibitor. 
|In vivo||In rabbits, SB225002 selectively blocks IL-8-induced neutrophil margination.  In mouse intrahepatic cholangiocellular carcinoma model, SB225002 (1 mg/kg i.p.) suppresses the growth of transplanted subcutaneous tumors.  In addition, SB225002 also displays long-lasting antinociceptive effects, and reduces TNBS-induced colitis in mouse models.  |
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.
-  White JR, et al. J Biol Chem. 1998, 273(17), 10095-10098.
-  Wang B, et al. Cancer Res. 2006, 66(6), 3071-3077.
-  Goda AE, et al. Biochem Pharmacol. 2013, 85(12), 1741-1752.
|In vitro||DMSO||70 mg/mL (198.78 mM)|
|Ethanol||3 mg/mL warmed (8.51 mM)|
|In vivo||Add solvents to the product individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
Whether the in vivo formulation for the drug: 2% DMSO/castor oil is a clear solution for injection or a suspension for oral administration?
S7651 can be dissolved in 2% DMSO/castor oil at 10 mg/ml as a clear solution and it is a suspension in 2% DMSO/30% PEG 300/dd H2O at 5 mg/mL.