Home GPCR & G Protein CXCR antagonist SB225002

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SB225002 CXCR2 antagonist

Cat.No.S7651

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 CXCR antagonist Chemical Structure

Chemical Structure

Molecular Weight: 352.14

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Quality Control

Cell Culture, Treatment & Working Concentration

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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 352.14 Formula

C13H10BrN3O4

 Storage (From the date of receipt)
CAS No. 182498-32-4 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC=C(C(=C1)NC(=O)NC2=C(C=C(C=C2)[N+](=O)[O-])O)Br

Solubility

In vitro
Batch:

DMSO : 70 mg/mL (198.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 14 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
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] This compound substantially reduces the levels of phosphorylated ERK1/2, and decreases cell proliferation in WHCO1 cells. [2] It 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.
In vivo
In rabbits, SB225002 selectively blocks IL-8-induced neutrophil margination. [1] In mouse intrahepatic cholangiocellular carcinoma model, this compound (1 mg/kg i.p.) suppresses the growth of transplanted subcutaneous tumors. [4] In addition, it also displays long-lasting antinociceptive effects, and reduces TNBS-induced colitis in mouse models. [5] [6]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/24582495/
  • [5] https://pubmed.ncbi.nlm.nih.gov/19264522/
  • [6] https://pubmed.ncbi.nlm.nih.gov/18653784/

Applications

Methods Biomarkers Images PMID
Western blot p-p53 / p53 p-Chk1 / Chk1 S7651-WB1 23359652
Growth inhibition assay Apoptosis S7651-viability1 23359652

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Frequently Asked Questions

Question 1:
Whether the in vivo formulation for it: 2% DMSO/castor oil is a clear solution for injection or a suspension for oral administration?

Answer:
It can be dissolved in 2% DMSO/castor oil at 10 mg/ml as a clear solution and is a suspension in 2% DMSO/30% PEG 300/dd H2O at 5 mg/mL.

Signaling Pathway Map