SB225002

Alias: SB225002; SB 225002; SB225002
Cat No.:V1490 Purity: ≥98%
SB225002 (SB 225002; SB-225002) is a novel, potent, and selective non-peptide antagonist of chemokine receptor CXCR2 with potential anti-inflammatory activity.
SB225002 Chemical Structure CAS No.: 182498-32-4
Product category: CXCR
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
500mg
Other Sizes
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text

 

  • Business Relationship with 5000+ Clients Globally
  • Major Universities, Research Institutions, Biotech & Pharma
  • Citations by Top Journals: Nature, Cell, Science, etc.
Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Purity: ≥98%

Product Description

SB225002 (SB 225002; SB-225002) is a novel, potent, and selective non-peptide antagonist of chemokine receptor CXCR2 with potential anti-inflammatory activity. It blocks the binding of interleukin 125I-IL-8 to CXCR2 and inhibits CXCR2 with an IC50 of 22 nM as well. More than 150 times as selective as CXCR1 and the other four 7-TMRs tested was demonstrated by SB 225002. The chemotaxis of human and rabbit neutrophils induced by IL-8 and GROalpha was potently inhibited in vitro by SB 225002. Rabbits' neutrophil margination caused by IL-8 was specifically inhibited in vivo by SB 225002. According to the current research, CXCR2 is in charge of IL-8-induced neutrophil chemotaxis and margination. It has also been reported that SB225002 functions as a mitotic inhibitor, independent of p53 status, to induce mitotic catastrophe in chemo-sensitive and -resistant ovarian cancer cells in vitro. By different means, SB225002 causes ovarian cancer (OVCA) cells with and without p53 to undergo apoptosis. This selective antagonist will be an effective tool in defining CXCR2's function in inflammatory diseases where neutrophils are important players.

Biological Activity I Assay Protocols (From Reference)
Targets
125I-IL-8-CXCR2 ( IC50 = 22 nM )
ln Vitro

In vitro activity: SB225002 effectively suppresses both IL-8 and GROalpha-induced human and rabbit neutrophil chemotaxis, as well as GROα-stimulated calcium mobilization.[1] In WHCO1 cells, SB 225002 significantly lowers the amounts of phosphorylated ERK1/2 and suppresses cell division.[2] Moreover, SB225002 exhibits antitumor activity by inhibiting microtubules.[3]

ln Vivo
SB225002 specifically inhibits the neutrophil margination induced by IL-8 in rabbits. [1] The growth of transplanted subcutaneous tumors is suppressed by SB225002 (1 mg/kg i.p.) in a mouse intrahepatic cholangiocellular carcinoma model. [4] Furthermore, SB225002 exhibits persistent antinociceptive properties and mitigates colitis induced by TNBS in mice models. [5] [6]
Enzyme Assay
There are ready membranes for CHO-CXCR1 and CHO-CXCR2. The experiments are carried out in 96-well microtiter plates with 1.0 μg/mL membrane protein in 20 mM Bis-Tris-propane, pH 8.0, and 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. Under standard binding conditions, the final Me2SO concentration is less than 1%. When 0.25 nM 125I-IL-8 (2,200 Ci/mmol) is added, binding is started. The plate is harvested onto a glass fiber filtermat blocked with 1% polyethyleneimine and 0.5% BSA after a one-hour incubation period at room temperature. The plate is then cleaned three times using 25 mM NaCl, 10 mM Tris•HCl, 1 mM MgSO4, 0.5 mMEDTA, 0.03% CHAPS, and pH 7.4. The filter is sealed in a sample bag with 10 mL of Wallac 205 Betaplate liquid scintillation fluid after it has dried, and a Wallac 1205 Betaplate liquid scintillation counter is used to count the results.
Cell Assay
Three esophageal squamous cell carcinoma cell lines—WHCO1, WHCO5, and WHCO6—are cultured in DMEM containing 10% FCS at 37°C in a humidified atmosphere with 5% CO2. These cell lines were initially established from surgical biopsies of primary esophageal squamous cell carcinomas. To perform MTT assays, use the Cell Proliferation kit. In 96-well plates, 1.5×103 cells are plated with a final volume of 180 μL DMEM per well. Cells are treated with 400 nM of SB 225002, and as a control, 0.001% DMSO (solvent) is added. Following the specified incubation time, each well receives 18 μL of the MTT labeling reagent (final concentration 0.5 mg/mL), which is then incubated for 4 hours in a humidified environment. The solubilization solution is poured into each well in a volume of 180,000 microliters, and the plates are then left at 37°C overnight. A microtiter plate reader is used to measure the samples' spectrophotometric absorbance at 595 nm.
Animal Protocol
Mice: Male 7-8 week old wildtype (C57BL/6J, Harlan) and ApoE−/− mice, raised on the same C57BL/6 background, are given a normal or cholesterol-rich diet for six weeks before having a left-sided middle cerebral artery occlusion (MCAO) for 20 minutes or having a sham operation performed. The treatment paradigms that animals receive are assigned at random, and experimenters are blinded throughout the entire intervention and data analysis process. Intraperitoneally (i.p.) injections of the vehicle (1% DMSO in PBS) or the selective CXCR2 antagonist SB225002 (2 mg/kg) are given at 0, 24, and 48 hours after ischemia. In additional studies, CXCR2 is blocked specifically by intraperitoneal injection (i.p.) of 300 μL of neutralizing rabbit anti-CXCR2 serum at 0 hours, 24 hours, and 48 hours after ischemia. NRS, or normal rabbit serum, was used as the control in the later investigations. In certain tests, an intraperitoneal injection of 200 μg anti-mouse Ly6G is used to deplete neutrophils 24 hours prior to and 24 hours following ischemia. 200 μg of an isotype control antibody are used as the control in these tests. Rats: For the purposes of this study, each dam produces 10–12 Sprague-Dawley rat pups. Injections of SB225002 (1 or 3 mg/kg) diluted in NS solution containing 0.33 % Tween 80, or vehicle (NS solution containing 0.33 % Tween 80) are given intraperitoneally to the pups 30 minutes prior to lipopolysaccharide (LPS) administration and right after hypoxic ischemia (HI). There are four groups of pups that are randomly assigned: vehicle (NS injections 30 minutes before LPS administration and immediately after HI, N=18), SB-1 (1 mg/kg, N=14) and SB-3 (3 mg/kg, N=18) (SB225002 injections 30 minutes before LPS administration and immediately after HI).
References

[1]. J Biol Chem . 1998 Apr 24;273(17):10095-8.

[2]. Cancer Res . 2006 Mar 15;66(6):3071-7.

[3]. Biochem Pharmacol . 2013 Jun 15;85(12):1741-52.

[4]. Surgery . 2014 Apr;155(4):640-9.

[5]. Eur J Pain . 2010 Jan;14(1):23-31.

[6]. J Leukoc Biol . 2008 Oct;84(4):1213-21.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C13H10BRN3O4
Molecular Weight
352.14
Exact Mass
350.99
Elemental Analysis
C, 44.34; H, 2.86; Br, 22.69; N, 11.93; O, 18.17
CAS #
182498-32-4
Appearance
White solid powder
SMILES
C1=CC=C(C(=C1)NC(=O)NC2=C(C=C(C=C2)[N+](=O)[O-])O)Br
InChi Key
MQBZVUNNWUIPMK-UHFFFAOYSA-N
InChi Code
InChI=1S/C13H10BrN3O4/c14-9-3-1-2-4-10(9)15-13(19)16-11-6-5-8(17(20)21)7-12(11)18/h1-7,18H,(H2,15,16,19)
Chemical Name
1-(2-bromophenyl)-3-(2-hydroxy-4-nitrophenyl)urea
Synonyms
SB225002; SB 225002; SB225002
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~70 mg/mL (~198.7 mM)
Water: <1 mg/mL
Ethanol: ~3 mg/mL warmed (~8.5 mM)
Solubility (In Vivo)
2%DMSO+Castor oil: 10mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8398 mL 14.1989 mL 28.3978 mL
5 mM 0.5680 mL 2.8398 mL 5.6796 mL
10 mM 0.2840 mL 1.4199 mL 2.8398 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • SB225002

    Competition binding of125I-IL-8, [3H]FMLP, [3H]LTB4, [3H]LTD4, or125I-C5a by SB 225002 to appropriate membranes expressing either cloned or primary receptors.1998 Apr 24;273(17):10095-8.

  • SB225002

    Effect of SB 225002 on IL-8-, GROα-, or C5a-induced human neutrophil chemotaxis.1998 Apr 24;273(17):10095-8.

  • SB225002

    Effect of SB 225002 on IL-8- and fMLP-induced neutrophil margination in rabbits.1998 Apr 24;273(17):10095-8.

Contact Us