assay
≥98% (HPLC)
Quality Segment
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)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable