Biochem/physiol Actions
Cell permeable: no
Reversible: no
Product does not compete with ATP.
Target IC50: 22 nM for the inhibition of 125I-IL-8 binding to CXCR2
General description
A potent and selective antagonist of G-protein coupled receptor CXCR2 (IL-8RB; IC50 = 22 nM for the inhibition of 125I-IL-8 binding to CXCR2). Inhibits human and rabbit neutrophil chemotaxis induced by both IL-8 and GROα in vitro and selectively blocks IL-8-induced neutrophil margination in rabbits. Reduces presenilin expression, inhibits γ-secretase activity, and blocks Aβ40/42 production and notch processing; further, demonstrates in vivo efficacy in mouse models.
A potent, selective, and competitive antagonist of the G-protein coupled receptor CXCR2 (IL-8RB; IC50 = 22 nM for the inhibition of 125I-IL-8 binding to CXCR2). Shows ~150-fold selectivity over CXCR1. Inhibits human and rabbit neutrophil chemotaxis induced by both IL-8 and GROα in vitro and in vivo selectively blocks IL-8-induced neutrophil margination in rabbits. Reduces presenilin expression, inhibits γ-secretase activity, and blocks Aβ40/42 production and notch processing; further, demonstrates in vivo efficacy in mouse models.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Bakshi, P., et al. 2009. ACS Chem. Biol.in press.White, J.R., et al. 1998. J. Biol. Chem. 273, 10095.
Packaging
Packaged under inert gas
1 mg in Glass bottle
Warning
Toxicity: Standard Handling (A)
This product has met the following criteria to qualify for the following awards: