Background:

SCH-527123 is a novel, selective CXC chemokine receptor 2 (CXCR2) antagonist.

SCH-527123 was able to suppress CXCR2-mediated signal transduction as shown through decreased phosphorylation of the NF-κB/mitogen-activated protein kinase (MAPK)/AKT pathway [1].?

Cells were treated with increasing concentrations of SCH-527123 for 72 hours and showed dose-dependent growth inhibitory activity with IC50 (72 h) values ranging from 18 to 40 μmol/L. Importantly the IL-8–overexpressing cells showed a higher IC50 (72 h) concentration of SCH-527123 than parental cells [HCT116 and E2 (P< 0.005): 28.9 ± 0.02 μmol/L and 39.5 ± 0.01 μmol/L, respectively; Caco2 and IIIe (P< 0.005): 18.8 ± 0.03 μmol/L and 25.5 ± 0.02 μmol/L, respectively]. Therefore, SCH-527123 decreased growth inhibitory activity in colorectal cancer cell lines [2].

参考文献

参考文献:
[1]. Holz O, Khalilieh S, Ludwig-Sengpiel A et al. SCH527123, a novel CXCR2 antagonist, inhibits ozone-induced neutrophilia in healthy subjects. Holz O1, Khalilieh S, Ludwig-Sengpiel A et al.
[2]. Holz O1, Khalilieh S, Ludwig-Sengpiel A et al. The CXCR2 antagonist, SCH-527123, shows antitumor activity and sensitizes cells to oxaliplatin in preclinical colon cancer models. Mol Cancer Ther. 2012 Jun;11(6):1353-64.