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Chemical Structure : BR0063
Catalog No.: PC-23344Not For Human Use, Lab Use Only.
BR0063 is a potent, selective EED-directed allosteric inhibitor of polycomb repressive complex 2 (PRC2), efficiently blocks the interaction of the EED subunit with H3K27me3 (EC50=5.9 nM), which led to the marked inhibition of cellular PRC2 activity.
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BR0063 is a potent, selective EED-directed allosteric inhibitor of polycomb repressive complex 2 (PRC2), efficiently blocks the interaction of the EED subunit with H3K27me3 (EC50=5.9 nM), which led to the marked inhibition of cellular PRC2 activity.
BR0063 effectively reduce the cellular H3K27me3 level with EC50 of 1-2 nM in panel of SWI/SNF LOF mutation cell lines.
BR0063 exhibits anti-proliferative effect of SWI/SNF mutation tumor cell lines DMS 114 and MFE-296 with EC50 of 10 nM.
BR0063 induces cell senescence or apoptosis in the sensitive cells.
BR0063 (10/80 mpk po bid) inhibits tumor growth in DMS 114 and MFE-296 xenograft models.
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| Appearance | Solid | |
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10 mM in DMSO |
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