Synonyms: BAY 1238097 | BAY-1238097
Compound class:
Synthetic organic
Comment: BAY1238097 is a BET inhibitor [1,3]. BET inhibitors bind to the bromodomains of the bromodomain and extra-terminal motif (BET) proteins BRD2, BRD3, BRD4, and BRDT. This mechanism acts to prevent protein-protein interaction between BET proteins and acetylated histones and transcription factors. The action disrupts chromatin remodeling and inhibits expression of some growth-promoting genes which slows proliferation in susceptible tumours.
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Bioactivity Comments |
An AACR meeting abstract (from AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA) reported an IC50 of <100 nM for BAY1238097 in a TR-FRET assay vs. BET BRD4 bromodomain 1 [2]. No bioactivity data for BAY1238097 has been published in a peer reviewed article (Nov 2016). |