SB225002

Catalog No.S7651

For research use only.

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

CAS No. 182498-32-4

Selleck's SB225002 has been cited by 57 publications

Purity & Quality Control

Choose Selective CXCR Inhibitors

Other CXCR Products

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 NUXsOZVwTnWwY4Tpc44h[XO|YYm= NYC2bGpkTGm|cHzhZ4Vu\W62IH;mJHsyOjWLXVnMPEBnem:vIHj1cYFvKHKnY3;tZolv[W62IFPYR3IzKGW6cILld5Nm\CCrbjDDTG8h[2WubIOsJGlEPTB;MkKgcm0> NF7VO2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{KzOlc3Oyd-MUeyN|Y4PjN:L3G+
human PMNs NILhfINHfW6ldHnvckBie3OjeR?= M1fwd2FvfGGpb37pd5Qh[WO2aY\peJkh[XRiQ2jDVlIhcW5iaIXtZY4hWE2QczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFPYR2wyNWmwZIXj[YQhcW62cnHj[YxtfWyjcjDDZVIsKHKnbHXhd4Uh[nliZnz1c5Jme2OnbnPlJIJie2WmIHPhcINqfW1iZnz1fEBie3OjeTygTWM2OD1|MDDuUS=> NHjOZWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK1OFY1OCd-MkWyOVQ3PDB:L3G+
HEK293 cells NYXxU25qTnWwY4Tpc44h[XO|YYm= M{XsTGFvfGGpb37pd5Qh[WO2aY\peJkh[XRiaIXtZY4hS1iFUkKg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFPYR2w5NWmwZIXj[YQhcW62cnHj[YxtfWyjcjDDZVIsKHKnbHXhd4Uh[nliZnz1c5Jme2OnbnPlJIJie2WmIHPhcINqfW1iZnz1fEBie3OjeTygTWM2OD12MDDuUS=> MkfXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NUS2OFAoRjJ3MkW0OlQxRC:jPh?=
CHO M2jmR2Z2dmO2aX;uJIF{e2G7 NU\0T4FbSW62YXfvcol{fCCjY4Tpeol1gSCjdDDDXGNTOiCneIDy[ZN{\WRiaX6gO5chS0iRIHPlcIx{KGOxLXX4dJJme3OrbnegbJVu[W5icnXjc41jcW6jboSgRXBRKDd3MTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\S2vZXTpZZRm\CCjbYnsc4llKGKndHG0NkBxem:mdXP0bY9vNCCLQ{WwJF0hOC53IN88UU4> NXfEN2gxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4OVM1PjFpPkG5PFU{PDZzPD;hQi=>
Assay
Methods Test Index PMID
Western blot p-p53 / p53 ; p-Chk1 / Chk1 23359652
Growth inhibition assay Apoptosis 23359652
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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[1]
  • Animal Models: Rabbits
  • Dosages: 5.5 μg/kg/min
  • Administration: Cannula in the external jugular vein

Solubility (25°C)

In vitro

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.

5mg/mL

Chemical Information

Molecular Weight 352.14
Formula

C13H10BrN3O4

CAS No. 182498-32-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C(=C1)NC(=O)NC2=C(C=C(C=C2)[N+](=O)[O-])O)Br

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

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.

Tags: buy SB225002 | SB225002 supplier | purchase SB225002 | SB225002 cost | SB225002 manufacturer | order SB225002 | SB225002 distributor