Description
SCH-527123 is a potent antagonist of both CXCR1 and CXCR2 with IC50 values of 42 nM and 3 nM, respectively.
Product Overview
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. 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.
Synonyms
SCH-527123; SCH527123
Targets
CXCR1/CXCR2 receptor
Molecular Formula
C21H23N3O5
Chemical Name
2-hydroxy-N,N-dimethyl-3-[[2-[[(1R)-1-(5-methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobuten-1-yl]amino]benzamide
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request