Biochem/physiol Actions

Blocking action of SB-225002 on CXCR2 (interleukin 8 receptor β), prevents the IL-8 induced matrix metalloproteinase-9 release from neutrophils. Matrix metalloproteinase-9 are proteolytic enzymes associated with inflammation.

SB-225002 is a potent nonpeptide inhibitor of chemokine receptor CXCR2 with an IC₅₀ of 22 nM for inhibiting interleukin IL-8 binding to CXCR2 and > 150-fold selectivity over CXCR1 receptors. CXCR2 binds many different immune cell chemoattractants. SB-225002 is crucial for cancer progression and is involved in inflammatory diseases like COPD, rheumatoid arthritis, and ulcerative colitis.

Features and Benefits

This compound is featured on the Chemokine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Packaging

5, 25 mg in glass bottle