Name: SCH 527123
Price: 312.00 USD

- Overview
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    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].
    
    [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.
- Properties
  - Categories
    
    CXCR1 and CXCR2 receptors antagonist
    
    Alternative Name
    
    SCH-527123;SCH527123; 2-hydroxy-N,N-dimethyl-3-[[2-[[(1R)-1-(5-methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobuten-1-yl]amino]benzamide
    
    CAS Number
    
    473727-83-2
    
    Molecular Formula
    
    C21H23N3O5
    
    Molecular Weight
    
    397.42
    
    Appearance
    
    A solid
    
    Purity
    
    99.20%
    
    Solubility
    
    insoluble in H2O; ≥103 mg/mL in EtOH with ultrasonic; ≥19.85 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CCC(C1=CC=C(O1)C)NC2=C(C(=O)C2=O)NC3=CC=CC(=C3O)C(=O)N(C)C
    
    * For Research Use Only
- Reference
  - 1. Ravi Holani, Anshu Babbar, et al. "Cathelicidin-mediated lipopolysaccharide signaling via intracellular TLR4 in colonic epithelial cells evokes CXCL8 production." Gut Microbes. 2020 Nov 9;12(1):1785802. PMID:32658599
    2. Ian Johnston. "Platelet Factor 4 And Von Willebrand Factor Form An Immunogenic, Prothrombotic Complex In Heparin-Induced Thrombocytopenia." University of Pennsylvania.2018.
    3. Ravi Holani, Fernando Lopes, et al. "Cathelicidin senses enteric pathogen Salmonella typhimurium/LPS for colonic chemokine generation: a new innate immune role for a host defense peptide." bioRxiv. 2018.
    4. Jinghua Jiang , Fei Ye, et al. "Peri-tumor associated fibroblasts promote intrahepatic metastasis of hepatocellular carcinoma by recruiting cancer stem cells." Cancer Letters.17 July 2017 1/10.
    5. Khanam A, Trehanpati N, et al. "Blockade of Neutrophil's Chemokine Receptors CXCR1/2 Abrogate Liver Damage in Acute-on-Chronic Liver Failure." Front Immunol. 2017 Apr 24;8:464. PMID:28484461
    6. Giannou AD, Marazioti A, et al. "NRAS destines tumor cells to the lungs." EMBO Mol Med. 2017 May;9(5):672-686. PMID:28341702