QNZ (EVP4593)

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    EVP4593 is an inhibitor of NF-κB pathway with IC50 value of 11nM [1].
    EVP4593 is a quinazoline derivative. It is screened out from a luciferase reporter gene-based assay using human Jurkat T cells. EVP4593 is found as an inhibitor of PMA/PHA-induced NF-κB pathway. It shows significant inhibition of both NF-κB transcriptional activation and TNF-α production (IC50 value of 7nM). Additionally, EVP4593 also has anti-inflammatory efficacy. It inhibits edema formation in a rat carrageenin-induced paw edema model [1].
    Since NF-κB pathway may play a direct role in Huntington’s disease (HD) pathogenesis, EVP4593 is found to have beneficial effects in Drosophila HD transgenic model. It significantly slows the progressive decline in the climbing speed without toxic effects [2].
    
    [1] Tobe M, Isobe Y, Tomizawa H, Nagasaki T, Takahashi H, Fukazawa T, Hayashi H. Discovery of quinazolines as a novel structural class of potent inhibitors of NF-kappa B activation. Bioorg Med Chem. 2003 Feb 6;11(3):383-91.
    [2] Wu J, Shih HP, Vigont V, Hrdlicka L, Diggins L, Singh C, Mahoney M, Chesworth R, Shapiro G, Zimina O, Chen X, Wu Q, Glushankova L, Ahlijanian M, Koenig G, Mozhayeva GN, Kaznacheyeva E, Bezprozvanny. Neuronal store-operated calcium entry pathway as a novel therapeutic target for Huntington's disease treatment. Chem Biol. 2011 Jun 24;18(6):777-93.
- Properties
  - Alternative Name
    
    4-N-[2-(4-phenoxyphenyl)ethyl]quinazoline-4,6-diamine
    
    CAS Number
    
    545380-34-5
    
    Molecular Formula
    
    C22H20N4O
    
    Molecular Weight
    
    356.42
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥10.06 mg/mL in EtOH with ultrasonic; ≥15.05 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Yen TH, Hsieh CL, et al. "Amentoflavone Induces Apoptosis and Inhibits NF-ĸB-modulated Anti-apoptotic Signaling in Glioblastoma Cells." In Vivo. 2018 Mar-Apr;32(2):279-285. PMID:29475910
    2. YU-CHANG LIU, RENG-HONG WU, et al. "Regorafenib diminishes the expression and secretion of angiogenesis and metastasis associated proteins and inhibits cell invasion via NF-κB inactivation in SK-Hep1 cells."Received February 19, 2016; Accepted January 12, 2017

QNZ (EVP4593)

Background

We Also Recommend

Birinapant (TL32711)

GDC-0152

YM155