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 MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Primary Target: CXCR2
530730
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₂H₂₄N₂OS

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.30730.0001
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          		 Glass bottle 10 mg
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          Description
          OverviewA 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

          Documentation

          CXCR2 Antagonist III, CX4338 - Calbiochem SDS

          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 +2°C to +8°C
          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.
          Toxicity Standard Handling
          ReferencesHa, H., et al. 2014. Bri. Journ. Pharm. 171, 1551.