CPI-637 |
Catalog No.GC10382 |
CPI-637 es un inhibidor selectivo y potente del bromodominio CBP/EP300 con valores IC50 de 0,03 μM, 0,051 μM y 11,0 μM para CBP, EP300 y BRD4 BD-1, respectivamente, y una EC50 de 0,3 μM para CBP.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1884712-47-3
Sample solution is provided at 25 µL, 10mM.
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.
Reference:
[1] Taylor, A. M. et al. Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637). ACS medicinal chemistry letters 7, 531-536, doi:10.1021/acsmedchemlett.6b00075 (2016).
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