Potent BET Bromodomain Inhibitor

OTX 015 is a potent inhibitor of BET (bromodomain and extra-terminal motif) bromodomain proteins including BRD2, BRD3 and BRD4. BET bromodomain protein, called “reader” in epigenetics, recognizes acetylated lysines in histones and regulates chromatin remodeling and transcription.¹⁾ Inhibition of these functions by OTX 015 decreases expression of an oncogene product MYC and negatively regulates signaling pathways of TLR, JAK/STAT, and important factors of immune response like NF-κB.²⁾ IC₅₀ of OTX 015 to BET bromodomain proteins ranges from 92 nM to 112 nM, indicating strong binding,³⁾ so OTX 015 is valuable for cancer and immune/inflammatory research.