Skip to main content
An official website of the United States government
Government Funding Lapse
Because of a lapse in government funding, the information on this website may not be up to date, transactions submitted via the website may not be processed, and the agency may not be able to respond to inquiries until appropriations are enacted.

The NIH Clinical Center (the research hospital of NIH) is open. For more details about its operating status, please visit cc.nih.gov.

Updates regarding government operating status and resumption of normal operations can be found at opm.gov.

EED inhibitor BR1733

An orally bioavailable inhibitor of the polycomb repressive complex 2 (PRC2) component embryonic ectoderm development (EED) protein, with potential antineoplastic activity. Upon oral administration, EED inhibitor BR1733 targets and binds to EED. This inhibits the binding of EED with trimethylated histone H3 on lysine 27 (H3K27me3), prevents the interaction of EED with the histone methyltransferase (HMT) and the catalytic subunit of the PRC2 enhancer zeste homolog 2 (EZH2), and prevents H3K27 methylation. The decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased tumor cell proliferation in EZH2-mutated and PRC2-dependent cancer cells. EZH2 is overexpressed or mutated in a variety of cancer cells. EED is essential for the histone methyltransferase activity of PRC2.
Check for active clinical trials using this agentView this agent in the NCI Thesaurus
Code name:BR 1733
BR-1733
BR1733
Search NCI's Drug Dictionary
Please enter up to 30 characters for your search