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SB225002 is a potent and selective non-peptide inhibitor of CXCR2 with IC50 of 22 nM and >150-fold selectivity over CXCR1 and four other 7-TMRs. SB225002 inhibits IL-8- (IC50=8nM) and GROα-mediated (IC50=10nM) calcium mobilisation. SB225002 prevents IL-8-induced neutrophil migration. SB225002 inhibits HIV replication in lymphocytes and macrophages. SB 225002 potently inhibited human and rabbit neutrophil chemotaxis induced by both IL-8 and GROalpha.
Patent. CN120425042A 2025 Aug 05; .
Patent. CN120425042A
SB225002 purchased from AbMole
BioRxiv. 2023 Oct 26;564292.
MIF Regulates M1 Macrophage Polarization via CD74/CXCR2/JNK Pathway and Mediates Aortic Dissection in Mice
SB225002 purchased from AbMole
Brain Res Bull. 2017 Jul 10;134:91-98.
The effect of CXCR2 inhibition on seizure activity in the pilocarpine epilepsy mouse model
SB225002 purchased from AbMole
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Source | Brain Research Bulletin (2017). Figure 4. SB225002 (Abmole Bioscience Inc., USA) |
| Method | Western blotting | |
| Cell Lines | TLE mice | |
| Concentrations | 2 mg/kg | |
| Incubation Time | 14 consecutive days | |
| Results | To further investigate the role of CXCR2 in epilepsy, we measured the effect of SB225002 on SRSs during the chronic period in the pilocarpine-induced epilepsy mice. The latency period of SRSs was increased (by nearly 40%) in the SB225002 group as compared with the model control and vehicle groups (p < 0.05). |
| Cell Experiment | |
|---|---|
| Cell lines | WHCO1, WHCO5, and WHCO6 cell lines |
| Preparation method | Establishing three esophageal squamous cell carcinoma cell lines WHCO1, WHCO5, and WHCO6 originally from surgical biopsies of primary esophageal squamous cell carcinomas which are cultured in DMEM containing 10% FCS at 37°C in a humidified atmosphere of 5% CO2.Using the Cell Proliferation kit I to carry out MTT assays . Briefly, plating 1.5 × 103 cells in 96-well plates in a final volume of 180 μL DMEM per well.Adding SB 225002 (antagonist of CXCR2, 400 nM)to cells and adding 0.001% DMSO (solvent) as a control. After the indicated incubation period, adding 18 μL of the MTT labeling reagent (final concentration 0.5 mg/mL)to each well and incubating for 4 hours in a humidified atmosphere. Adding one hundred eighty microliters of the solubilization solution to each well and the plates were left overnight at 37°C. Using a microtiter plate reader to measure the spectrophotometric absorbance of samples at 595 nm . |
| Concentrations | 400 nM |
| Incubation time | 6 days |
| Animal Experiment | |
|---|---|
| Animal models | Rabbits |
| Formulation | DMSO |
| Dosages | 5.5 μg/kg/min |
| Administration | Cannula in the external jugular vein |
| Molecular Weight | 352.14 |
| Formula | C13H10BrN3O4 |
| CAS Number | 182498-32-4 |
| Solubility (25°C) | DMSO ≥ 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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|---|
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Plerixafor (AMD3100) is a CXCR4 chemokine receptor antagonist. |
| WZ 811
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| Navarixin
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| AMD3465 hexahydrobromide (AMD3465 )
AMD3465 hexahydrobromide（AMD3465 ) is an effective CXCR4 antagonist that inhibits 12G5 mAb in SupT1 cells. The IC50 values of CXCL12AF647 and CXCR4 were 0.75 nM and 18 nM, respectively. AMD 3465 also effectively inhibited X4 HIV replication (IC50, 1-10 nM), but not R5 HIV replication. |
| Plerixafor 8HCl
Plerixafor 8HCl (AMD3100 8HCl) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively. |
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