ezh2 in 5

EZH2-IN-5 is a highly effective inhibitor of EZH2, displaying remarkable potency against both wild-type and mutant Tyr641 EZH2, with IC50 values of 1.52 nM and 4.07 nM, respectively.

PROTAC EZH2 Degrader-3（化合物ZJ-20）是一种有效的EZH2降解剂。在5 μM浓度和24小时处理下，此化合物不仅显著抑制EZH2蛋白的表达，还强烈抑制PRC2复合体中其他亚基以及H3k27me3蛋白的表达。此外，PROTAC EZH2 Degrader-3展现出抗增殖活性，能够阻断细胞周期在G0-G1期并诱导细胞凋亡（apoptosis）。

EZH2-IN-4 is a highly potent EZH2 inhibitor that can be taken orally. It exhibits inhibitory effects against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, with IC 50 values of 0.923 nM and 2.65 nM, respectively. Moreover, EZH2-IN-4 has demonstrated significant anti-cancer activity.

EZH2-IN-12 (Compound 5) 是一种 EZH2 的有效抑制剂。EZH2-IN-12 具有潜力进行中枢神经系统恶性肿瘤的研究。