ezh2-in-3

EZH2-IN-3 is an inhibitor of EZH2 and EZH1 with selective impact on diffuse large B cell lymphoma cell growth.

3-Deazaneplanocin A (DZNep) is a dual inhibitor of histone methyltransferase (EZH2) and S-adenosylhomocysteine hydrolase (AHCY) with antipoxidative activity that inhibits hepatic, renal, peritoneal, and airway fibrosis by inducing proteasomal degradation of its targets and reducing toxicity in animal models.

PROTAC EZH2 Degrader-3 (compound ZJ-20) is a potent EZH2 degrader that exhibits strong inhibitory effects not only on EZH2 protein expression but also on the levels of other PRC2 subunits and H3k27me3 protein. Additionally, PROTAC EZH2 Degrader-3 demonstrates antiproliferative activity by blocking the cell cycle at the G0-G1 phase and inducing apoptosis (cell death). At a concentration of 5 μM and over a period of 24 hours, it effectively suppresses the expression of these critical proteins involved in cell regulation and growth.