PRC2 EED-IN-1

Names

[ Name ]:
PRC2 EED-IN-1

Biological Activity

[Description]:

PRC2 EED-IN-1 is a potent, selective, allosteric, orally bioavailable inhibitor of the EED subunit of histone methyltransferase PRC2 with IC50 of 44 nM (H3K27me3 inhibition).PRC2 EED-IN-1 retains efficacy against EZH2 inhibitor-resistant cell lines (Karpas 44 cell IC50=27 nM), exhibits in vivo efficacy in EZH2-driven tumors in vivo.

[References]

1. Bagal SK, et al. J Med Chem. 2021 Dec 9;64(23):17146-17183.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₉H₁₉FN₈O

[ Molecular Weight ]:
394.414

Related Compounds

IL-15-IN-1
Hsp90-Cdc37-IN-1
TLR7/8-IN-1
B-Raf IN 1
O-glycosylation-IN-1
T338C Src-IN-1
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3-{5-[(2,6-Dimethylpiperidin-1-yl)methyl]thiophen-3-yl}prop-2-yn-1-ol
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