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530730 CXCR2 Antagonist III, CX4338 - Calbiochem

530730
  
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₂H₂₄N₂OS
Description
Overview

This product has been discontinued.



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.

Catalogue Number530730
Brand Family Calbiochem®
References
ReferencesHa, H., et al. 2014. Bri. Journ. Pharm. 171, 1551.
Product Information
FormPale yellow solid
Hill FormulaC₂₂H₂₄N₂OS
Chemical formulaC₂₂H₂₄N₂OS
Quality LevelMQ100
Applications
Biological Information
Primary TargetCXCR2
Primary Target IC<sub>50</sub>6.3 µM
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
530730 0

Documentation

CXCR2 Antagonist III, CX4338 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Ha, H., et al. 2014. Bri. Journ. Pharm. 171, 1551.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision27-June-2014 JSW
DescriptionA cyclohexenone based compound that selectively inhibits CXCR2-mediated recruitment of ?-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.
FormPale yellow solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₂H₂₄N₂OS
Purity≥98% by HPLC
SolubilityDMSO (25 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesHa, H., et al. 2014. Bri. Journ. Pharm. 171, 1551.