SB225002

Catalog No.S7651

SB225002 Chemical Structure

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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4 Customer Reviews

  • 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.

    SB225002 could inhibited h-JBMMSCs chemotaxis in both the co-culture and the monoculture transwell systems (n = 3; *P < 0.05).

    J Cell Mol Med, 2017. 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

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Biological Activity

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.
Targets
CXCR2 [1]
(Cell-free assay)
22 nM
In vitro

In vitro, SB225002 inhibits GROα-stimulated calcium mobilization, and potently inhibits human and rabbit neutrophil chemotaxis induced by both IL-8 and GROalpha. [1] SB 225002 substantially reduces the levels of phosphorylated ERK1/2, and decreases cell proliferation in WHCO1 cells. [2] SB225002 also shows the antitumor activity as a microtubule inhibitor. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO cells NHL6eJVHfW6ldHnvckBie3OjeR?= NHezWIFFcXOybHHj[Y1mdnRib3[gX|EzPUmfSVy4JIZzd21iaIXtZY4hemWlb33ibY5idnRiQ2jDVlIh\XiycnXzd4VlKGmwIFPIU{Bk\WyuczygTWM2OD1{MjDuUS=> M2PHNFE4OjN4N{[z
human PMNs NHTnfYJHfW6ldHnvckBie3OjeR?= NEPBTW9CdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFPYR3IzKGmwIHj1cYFvKFCPToOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDDXGNNOS2rbnT1Z4VlKGmwdILhZ4VtdHWuYYKgR4EzMyC{ZXzlZZNmKGK7IH\seY9z\XOlZX7j[UBj[XOnZDDjZYxkcXWvIH\seZgh[XO|YYmsJGlEPTB;M{Cgcm0> MYWyOVI2PDZ2MB?=
HEK293 cells NUT6VGROTnWwY4Tpc44h[XO|YYm= MYPBcpRi\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJGNZS1J{IHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCFWFPMPE1qdmS3Y3XkJIlvfHKjY3XscJVt[XJiQ3GyL{Bz\WynYYPlJIJ6KG[udX;y[ZNk\W6lZTDiZZNm\CClYXzjbZVuKG[udYigZZN{[XluIFnDOVA:PDBibl2= M4i1OVI2OjV2NkSw

... Click to View More Cell Line Experimental Data

In vivo In rabbits, SB225002 selectively blocks IL-8-induced neutrophil margination. [1] In mouse intrahepatic cholangiocellular carcinoma model, SB225002 (1 mg/kg i.p.) suppresses the growth of transplanted subcutaneous tumors. [4] In addition, SB225002 also displays long-lasting antinociceptive effects, and reduces TNBS-induced colitis in mouse models. [5] [6]

Protocol

Kinase Assay:[1]
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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.
Cell Research:[2]
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  • Cell lines: WHCO1, WHCO5, and WHCO6 cell lines
  • Concentrations: 400 nM
  • Incubation Time: 6 days
  • Method: 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)
Animal Research:[1]
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  • Animal Models: Rabbits
  • Formulation: DMSO
  • Dosages: 5.5 μg/kg/min
  • Administration: Cannula in the external jugular vein
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 70 mg/mL (198.78 mM)
Ethanol 3 mg/mL warmed (8.51 mM)
Water Insoluble
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
5mg/mL

* 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.

Chemical Information

Molecular Weight 352.14
Formula

C13H10BrN3O4

CAS No. 182498-32-4
Storage powder
Synonyms N/A

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Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    Whether the in vivo formulation for the drug: 2% DMSO/castor oil is a clear solution for injection or a suspension for oral administration?

  • Answer:

    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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID