Home Bromodomain BET/Warhead Ligand
Lysine acetylation creates binding sites for the epigenetic reader domains of BET bromodomain proteins, which have emerged as key regulators of lineage-specific gene transcription. The development of potent and highly selective inhibitors, widely available in a short period, has facilitated mechanistic studies across various disease models, leading to rapid translation into clinical applications. Initial investigations into pan-BET inhibitors have now progressed to second-generation inhibitors with improved domain selectivity, as well as highly potent bifunctional and dual inhibitors, expanding the toolkit for fundamental research on acetylation-dependent transcription, diseases associated with BET, and further translational endeavors targeting this intriguing family of epigenetic reader domains.
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