BR-001 | PRC2 EED inhibitor | Probechem Biochemicals

Chemical Structure : BR-001

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BR-001 (BR001)

货号: PC-73067Not For Human Use, Lab Use Only.

BR-001 (BR001) is a potent, selective, allosteric inhibitor of EED subunit of PRC2 complex, disrupts EED-H3K27me3 interaction (IC50=4.5 nM).

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生物&药学活性

BR-001 (BR001) is a potent, selective, allosteric inhibitor of EED subunit of PRC2 complex, disrupts EED-H3K27me3 interaction (IC50=4.5 nM).
BR-001 directly binds to EED in the H3K27me3-binding pocket, BR-001 significantly increases the thermal stability of EED in thermal shift assay.
BR-001 is selective for EED, has no activity against 371 wild-type kinases.
BR-001 significantly reduced the cellular H3K27me3 level and also exhibited a strong antiproliferative effect in Karpas 422 cells.
BR-001 inhibited proliferation of DLBCL cells and tumor growth, and upregulated target genes expression.
BR-001 has potent antitumor efficacy in vivo, modulates immune response to suppress syngeneic CT26 colon tumor.

物理化学性质&存储条件

分子量	368.409
分子式	C20H17D2FN4O2
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	2-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl-d2)amino)-3-methyl-5-(2-methylpyridin-3-yl)pyrimidin-4(3H)-one

参考文献

1. Dong H, et al. Cancer Res. 2019 Nov 1;79(21):5587-5596.

BR-001 (BR001)

生物&药学活性

物理化学性质&存储条件

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BR-001 (BR001)

生物&药学活性

物理化学性质&存储条件

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