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)