CX4338
CX4338 is a CXCL8-mediated chemokine inhibitor with the activity of inhibiting CXCR2-mediated cell migration. CX4338 selectively inhibits CXCR2-mediated β-arrestin-2 recruitment and receptor internalization while enhancing CXCR2-mediated MAPK activation. CX4338 also inhibited CXCL8-induced chemotaxis, showing efficacy in CXCR2-overexpressing cells and human neutrophils. In vivo, CX4338 significantly reduced LPS-induced neutrophil numbers in mouse bronchoalveolar lavage fluid. The mechanism of action of CX4338 is to selectively inhibit CXCR2-mediated β-arrestin-2 activation, which is sufficient to inhibit CXCL8-mediated chemotaxis.
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- CAS No.: 41609-06-7
- Formule: C22H24N2OS
- Masse moléculaire:364.50
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U2OS | IC50 |
6.3 μM
Compound: 35; CX4338
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Antagonist activity at CXCR2 in human U2OS cells assessed as effect on beta-arrestin2 recruitment by CCF4-AM staining based Tango assay
Antagonist activity at CXCR2 in human U2OS cells assessed as effect on beta-arrestin2 recruitment by CCF4-AM staining based Tango assay
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[PMID: 31732253] |
Chemical Information
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CAS No. 41609-06-7
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Masse moléculaire 364.50
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Formule C22H24N2OS
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SMILES
O=C1CC(C)(CC(NCC2=CC=CC=C2)=C1C(NC3=CC=CC=C3)=S)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)