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).
Synonym(s):
SB 225002, N-(2-Hydroxy-4-nitrophenyl)-Nʹ-(2-bromophenyl)urea, CXCR2 Antagonist II
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.
Biochem/physiol Actions
Cell permeable: no
Product does not compete with ATP.
Reversible: no
Target IC50: 22 nM for the inhibition of 125I-IL-8 binding to CXCR2
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Other Notes
Bakshi, P., et al. 2009. ACS Chem. Biol.in press. White, J.R., et al. 1998. J. Biol. Chem. 273, 10095.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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