Name: EI1
Price: 282.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    IC50: A potent and selective suppressor of Ezh2 with IC50 values of 15 nM and 13 nM for wild type Ezh2 and Ezh2 Y641F mutant, respectivelyEI1 performs as a highly potent inhibitor of Ezh2 which is named enhancer of zeste homolog 2. Mutation and over-expression of Ezh2 has been linked to the development of cancer. Since Ezh2 is upregulated in multiple cancers, it seems to play a crucial role in the regulation of tumor angiogenesis and has been considered as a potential target in anticancer therapy. Ezh2 stimulates cancer development by inhibiting tumor-suppressing genes. Suppressing Ezh2 activity may therefore inhibit tumor growth. [1] In vitro: Based on studies from DLBCL cells, it was shown that EI1 suppressed cellular H3K27 methylation and activated expression of Ezh2 target gene - p16. EI1 also blocked H3K27 methylation and cell proliferation in mouse embryonic fibroblasts. In addition, EI1 potently and selectively inhibited the growth of DLBCL cells carrying Ezh2 mutation, and therefore resulted in cell cycle arrest and apoptosis. [1]In vivo: So far, no in vivo study has been conducted.Clinical trial: So far, no clinical trial has been conducted.
- Properties
  - Alternative Name
    
    6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide
    
    CAS Number
    
    1418308-27-6
    
    Molecular Formula
    
    C23H26N4O2
    
    Molecular Weight
    
    390.48
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥19.5 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

EI1

EI1

Background

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