Home GPCR & G Protein CXCR antagonist SB225002 For research use only.

SB225002

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.

SB225002 Chemical Structure

SB225002 Chemical Structure

CAS No. 182498-32-4

Purity & Quality Control

SB225002 Related Products

Signaling Pathway

CXCR Signaling Pathways

CXCR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO cells Function assay Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cells, IC50=22 nM 17236763
human PMNs Function assay Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay, IC50=30 nM 25254640
HEK293 cells Function assay Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assay, IC50=40 nM 25254640
CHO Function assay Antagonist activity at CXCR2 expressed in 7w CHO cells co-expressing human recombinant APP 751 assessed as inhibition of gamma-secretase-mediated amyloid beta42 production, IC50 = 0.5 μM. 19853461
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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 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]
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.
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-p53 / p53 p-Chk1 / Chk1 23359652
Growth inhibition assay Apoptosis 23359652
In Vivo
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]
Animal Research Animal Models Rabbits
Dosages 5.5 μg/kg/min
Administration Cannula in the external jugular vein

Chemical Information & Solubility

Molecular Weight 352.14 Formula

C13H10BrN3O4
CAS No. 182498-32-4 SDF Download SB225002 SDF
Smiles C1=CC=C(C(=C1)NC(=O)NC2=C(C=C(C=C2)[N+](=O)[O-])O)Br
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 70 mg/mL ( (198.78 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 14 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

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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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