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.
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
|Source||Brain Research Bulletin (2017). Figure 4. SB225002 (Abmole Bioscience Inc., USA)|
|Cell Lines||TLE mice|
|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 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 .|
|Incubation time||6 days|
|Administration||Cannula in the external jugular vein|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 35 mg/mL|
A growth-related oncogene/CXC chemokine receptor 2 autocrine loop contributes to cellular proliferation in esophageal cancer.
Wang B, et al. Cancer Res. 2006 Mar 15;66(6):3071-7. PMID: 16540656.
Characterization of the molecular interactions of interleukin-8 (CXCL8), growth related oncogen alpha (CXCL1) and a non-peptide antagonist (SB 225002) with the human CXCR2.
Catusse J, et al. Biochem Pharmacol. 2003 Mar 1;65(5):813-21. PMID: 12628493.
Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration.
White JR, et al. J Biol Chem. 1998 Apr 24;273(17):10095-8. PMID: 9553055.
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SX-682 is a potent and selective CXCR1/2 allosteric inhibitor, it may be useful for castration-resistant prostate cancer.
VUF11207 fumarate is a CXCR7 agonist and a high-potency CXCR7 ligand (pKi=8.1).
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