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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-BR0063
BR0063

Chemical Structure : BR0063

CAS No.:

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BR0063 (BR-0063)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量
分子式
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

参考文献

1. Xinghao Wang, et al. Cell Death Dis. 2024 Nov 5;15(11):794.

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