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530730 CXCR2 Antagonist III, CX4338 - Calbiochem

A selective inhibitor of CXCR2-mediated recruitment of β-arrestin-2 (IC₅₀ = 6.3 µM).

CXCR2 Antagonist III, CX4338 - Calbiochem : FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.
Primary Target: CXCR2
530730
  
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      Aperçu

      Replacement Information

      Tableau de caractéristiques principal

      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
      Référence GTIN
      530730 0

      Documentation

      CXCR2 Antagonist III, CX4338 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Ha, H., et al. 2014. Bri. Journ. Pharm. 171, 1551.
      Fiche technique

      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.