Name: YK-4-279
Price: 180.00 USD

- Overview
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    Background
    
    YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding to the oncogenic transciption factor EWS-FLI1.
    EWS-FLI1 is a disordered protein that precludes standard structure-based small-molecule inhibitor design. EWS-FLI1 binding to RNA helicase A (RHA) is important for its oncogenic function.
    In vitro: ESFT cells treated with YK-4-279 showed a dissociation of EWS-FLI1 from RHA by 10 mM, consistent with the KD value. The EWS-FLI1–transfected cells showed a dose-dependent decrease in promoter activity when treated for 18 h with 3 mM and 10 mM YK-4-279. YK-4-279 was relatively specific for ESFT cells as compared to the nontransformed HEK293 cells [1].
    In vivo: The tumor growth rate of YK-4-279–treated mice bearing CHP-100 was lower than that in mice having PC3 prostate tumors. The cumulative data from five independent experiments with the ESFT xenografts (TC71 and CHP-100) show a marked overall tumor reduction in the YK-4-279–treated mice. Pathological analysis of mice treated with YK-4-279 did not show any signs of toxicity, except for sterile inflammatory lesions in the abdominal cavities of mice [1].
    Clinical trial: No clinical data are available currently.
- Properties
  - Alternative Name
    
    YK 4-279; 4,7-dichloro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-1H-indol-2-one
    
    CAS Number
    
    1037184-44-3
    
    Molecular Formula
    
    C17H13Cl2NO4
    
    Molecular Weight
    
    366.2
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥16.35 mg/mL in DMSO; ≥24.25 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

YK-4-279

YK-4-279

Background

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