559405
SB 225002
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
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About This Item
Empirical Formula (Hill Notation):
C13H10BrN3O4
CAS Number:
Molecular Weight:
352.14
MDL number:
UNSPSC Code:
51111800
NACRES:
NA.77
Quality Level
Assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
yellow
solubility
DMSO: 200 mg/mL
shipped in
ambient
storage temp.
−20°C
SMILES string
Brc1c(cccc1)NC(=O)Nc2c(cc(cc2)[N+](=O)[O-])O
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.
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.
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)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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