For research use only.

Catalog No.S7651

44 publications

SB225002 Chemical Structure

CAS No. 182498-32-4

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.

Selleck's SB225002 has been cited by 44 publications

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.
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 NG\OZXNHfW6ldHnvckBie3OjeR?= NIDEVFNFcXOybHHj[Y1mdnRib3[gX|EzPUmfSVy4JIZzd21iaIXtZY4hemWlb33ibY5idnRiQ2jDVlIh\XiycnXzd4VlKGmwIFPIU{Bk\WyuczygTWM2OD1{MjDuUS=> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzJ|Nke2N{c,OTd{M{[3OlM9N2F-
human PMNs NUP6bHpxTnWwY4Tpc44h[XO|YYm= NWnOfmdjSW62YXfvcol{fCCjY4Tpeol1gSCjdDDDXGNTOiCrbjDoeY1idiCSTV7zJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gR3hEVDFvaX7keYNm\CCrboTyZYNmdGy3bHHyJGNiOiticnXs[YF{\SCkeTDmcJVwemW|Y3XuZ4Uh[mG|ZXSgZ4Ft[2m3bTDmcJV5KGG|c3H5MEBKSzVyPUOwJI5O MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ3NE[0NEc,OjV{NUS2OFA9N2F-
HEK293 cells M2HVOmZ2dmO2aX;uJIF{e2G7 M3rufGFvfGGpb37pd5Qh[WO2aY\peJkh[XRiaIXtZY4hS1iFUkKg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFPYR2w5NWmwZIXj[YQhcW62cnHj[YxtfWyjcjDDZVIsKHKnbHXhd4Uh[nliZnz1c5Jme2OnbnPlJIJie2WmIHPhcINqfW1iZnz1fEBie3OjeTygTWM2OD12MDDuUS=> M2rSWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkW0OlQxLz5{NUK1OFY1ODxxYU6=
CHO NVLacGFHTnWwY4Tpc44h[XO|YYm= M1HIRWFvfGGpb37pd5Qh[WO2aY\peJkh[XRiQ2jDVlIh\XiycnXzd4VlKGmwIEf3JGNJVyClZXzsd{Bkdy2neIDy[ZN{cW6pIHj1cYFvKHKnY3;tZolv[W62IFHQVEA4PTFiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UudWWmaXH0[YQh[W27bH;p[EBj\XSjNEKgdJJw\HWldHnvckwhUUN3MDC9JFAvPSEQvF2u NYfzR3E2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4OVM1PjFpPkG5PFU{PDZzPD;hQi=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-p53 / p53 ; 

PubMed: 23359652     

SB225002 (0–1000 nM, 24 h) increased total- and phospho-p53 (S15) level in OV2008, C13*, A2780s cells and increased phospho-p53 in A2780cp cells. SB225002 increased the phospho-p53/total-p53 ratio in all cell lines (Western blot). 

p-Chk1 / Chk1 ; 

PubMed: 23359652     

SB225002 (0–1000 nM, 24 h) decreased total and phospho-Chk1 (S317 and S345) levels in OV2008 cells.

Growth inhibition assay

PubMed: 23359652     

CDDP (0–10 µM, 24 h) induced apoptosis in chemo-sensitive OV2008 and A2780s but not their resistant counterparts C13* and A2780cp, whereas SB225002 (0–1000 nM, 24 h) induced apoptosis in all cell lines. The OVCAs were treated with different concentration of SB225002 or of CDDP for 24 h. The attached (viable) and floating (apoptotic) cells were pooled, washed and resuspended in neutral-buffered formalin (4%) containing Hoechst 33258 dye (3.75 ng/ml, 24 h). The percentage of apoptosis was determined based on nuclear morphology. At least 400 cells were counted in each group and the counter “blinded” to sample identity to avoid experimental bias.

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]


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
  • 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 to the product individually and in order(Data is from Selleck tests instead of citations):
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.

Chemical Information

Molecular Weight 352.14


CAS No. 182498-32-4
Storage powder
in solvent
Synonyms N/A
Smiles C1=CC=C(C(=C1)NC(=O)NC2=C(C=C(C=C2)[N+](=O)[O-])O)Br

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

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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.

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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.

CXCR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID