(R)-OR-S1

A novel SAM-competitive, highly selective, orally bioavailable EZH1/2 dual inhibitor with IC50 of 16/50 nM, respectively; also inhibits EZH2 Y641N mutant (IC50=50 nM), shows no significant activity against a panel of 253 kinases; show greater antitumor efficacy than EZH2 selective inhibitor against KARPAS-422 cells harboring a GOF mutation in EZH2, also more potently reduced H3K27me3 in cells than EZH2 selective inhibitors.

References 1. Honma D, et al. Cancer Sci. 2017 Oct;108(10):2069-2078. View Related Products by Target Histone Methyltransferase (HMTase)