CPI-637

- Overview
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    Background
    
    IC50: 0.03 and 11.0 μM for CBP/EP300 and BRD4, respectively.CPI-637 is a CBP/EP300 bromodomain inhibitor. It has been reported that among bromodomain-containing proteins implicated in various disease pathways, cyclic-AMP response element binding protein (CBP) and adenoviral E1A binding protein of 300 kDa (EP300), which is a highly homologous pair of bromodomain-containing transcriptional coactivators, are of great interest as potential drug targets due to their reported involvement in a variety of disease states.In vitro: Previous study found that CPI-637 was potent against EP300, and its opposite enantiomer showed a over 200-fold loss in potency. Moreover, the biochemical potency of CPI-637 translated well into cells with CBP BRET EC50 of 0.3 μM, and CPI-637 demonstrated a more than 700-fold selectivity over the BET family of bromodomains. In addition, CPI-637 was also highly selective against other bromodomains, showing substantial biochemical activity only against BRD9. Furthermore, it was found that CPI-637 was able to inhibit the expression of MYC with an EC50 of 0.60 μM in a cellular assay,. [1]. In vivo: So far, there is no animal in vivo data reported. Clinical trial: Up to now, CPI-637 is still in the preclinical development stage.
- Properties
  - Alternative Name
    
    (S)-4-methyl-6-(1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl)-4,5-dihydro-1H-benzo[b][1,4]diazepin-2(3H)-one
    
    CAS Number
    
    1884712-47-3
    
    Molecular Formula
    
    C22H22N6O
    
    Molecular Weight
    
    386.45
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥19.3 mg/mL in DMSO with gentle warming
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

CPI-637

Background

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