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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.