A-395 (A395) is a potent, selective, and cellularly active PRC2 subunit EED inhibitor with Kd of 1.5 nM.
A-395 potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with IC50 of 18 nM, and inhibits PRC2 at 1 and 50 uM.
A-395 shows no activity against any of the other protein lysine methyltransferases, arginine methyltransferases, or DNA methyltransferases.
A-395inhibits both H3K27me2 and H3K27me3 with IC50 of 390 nM and 90 nM, respectively; exhibits potent antitumor efficacy in vivo.
