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BR0063

Chemical Structure : BR0063

CAS No.:

BR0063 (BR-0063)

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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt
Formula
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

References

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