Immunology & Inflammation
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CXCR2 ligand
SRT3109是一种CXCR2配体,用于治疗趋化因子介导的疾病和状况。
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CXCR2 拮抗剂
SB225002是一种有效的选择性CXCR2拮抗剂,IC50为22 nM,可抑制白介素IL-8与CXCR2的结合,选择性是其他测试的7-TMR的150倍以上。
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CXCR1/CXCR2 拮抗剂
SCH-527123 (Navarixin)是人CXCR1和CXCR2受体的强效选择性拮抗剂,IC50分别为42 nM和3 nM。
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- Ruijie Zhang, .et al. Combined inhibition of IL-6 and IL-8 pathways suppresses ovarian cancer cell viability and migration and tumor growth, Int J Oncol, 2022, May;60(5):50 PMID: 35315502
- Fu S, .et al. Inhibition of interleukin 8/C-X-C chemokine receptor 1,/2 signaling reduces malignant features in human pancreatic cancer cells, Int J Oncol, 2018, Jul;53(1):349-357 PMID: 29749433
- Fu S, .et al. Blocking Interleukin-6 and Interleukin-8 Signaling Inhibits Cell Viability, Colony-forming Activity, and Cell Migration in Human Triple-negative Breast Cancer and Pancreatic Cancer Cells, Anticancer Res, 2018, Nov;38(11):6271-6279 PMID: 30396947
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CXCR2 拮抗剂
AZD-5069是一种有效的选择性CXCR2拮抗剂,具有抑制COPD患者中性粒细胞向气管迁移的潜能。
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SIRT1 activator
SRT3190是一种强效cxcr2配体。
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CXCL8 receptor 抑制剂
Reparixin L-lysine salt是CXCL8受体的抑制剂,也抑制CXCR1和CXCR2的活化,已显示在各种损伤模型中减弱了炎症反应。
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CXCR2 拮抗剂
SB265610是CXCR2 (Kd = 2.51 nM)的非肽变构反向激动剂,通过与不同于激动剂结合位点的区域结合来防止受体活化。它不与相关CXCR1受体结合。在体外和高氧诱导肺损伤的大鼠模型中,它已被证明能防止中性粒细胞趋化性。
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CXCL8/CXCR1/2 抑制剂
Reparixin是两种CXCL8受体CXCR1/2的有效抑制剂,它抑制CXCR2介导的细胞迁移(IC50 = 100 nM),而它强烈地阻断CXCR1介导的趋化性(IC50 = 1 nM)。
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- Naour AL, .et al. Tumor cells educate mesenchymal stromal cells to release chemoprotective and immunomodulatory factors, J Mol Cell Biol, 2019, Sep 3 PMID: 31504643
- Wigenstam E, .et al. N-acetyl cysteine improves the effects of corticosteroids in a mouse model of chlorine-induced acute lung injury, Toxicology, 2015, Feb 3;328:40-7 PMID: 25497111
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CXCR2/CXCR1 拮抗剂
SCH 563705是有效的双重CXCR2(IC50 = 1.3 nM)/CXCR1(IC50 = 7.3 nM)拮抗剂。
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