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 番号: 41609-06-7
- 分子式: C22H24N2OS
- 分子量:364.50
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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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
|
[PMID: 31732253] |
化学情報
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CAS 番号 41609-06-7
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分子量 364.50
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)