5.30730
CXCR2 Antagonist III, CX4338
Synonym(s):
CXCR2 Antagonist III, CX4338
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About This Item
Empirical Formula (Hill Notation):
C22H24N2OS
Molecular Weight:
364.50
UNSPSC Code:
12352200
Assay
≥98% (HPLC)
Quality Level
form
solid
potency
6.3 μM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
pale yellow
solubility
DMSO: 25 mg/mL
storage temp.
2-8°C
General description
A cyclohexenone based compound that selectively inhibits CXCR2-mediated recruitment of β-arrestin-2 (IC50 = 6.3 µM) and receptor internalization in U2OS cells, but does not affectCXCL-8 mediated turnover of CXCR2. Believed to interact with the C-terminal region of CXCR2 in close proximity to the receptor phosphorylation sites. Its action appears to be non-competitive and allosteric in nature. Does not affect the activity of CXCR4 (IC50 >100 µM). Shown to transiently increase CXCL8 -induced ERK1/2 phosphorylation. Does not affect CXCL8-mediated cAMP signaling in 293T-CXCR2-GFP-p22F cells. Inhibits CXCL8-mediated cell migration in a wound healing assay and reduces polymorphonuclear leukocyte migration in a lipopolysaccharide-induced inflammation model.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Primary Target
CXCR2
CXCR2
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Ha, H., et al. 2014. Bri. Journ. Pharm.171, 1551.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
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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