PROTAC EZH2 Degrader-27 

PROTAC EZH2 Degrader-27 is a EZH2 PROTAC inhibitor with an IC₅₀ of 4.00 nM against EZH2. PROTAC EZH2 Degrader-27 inhibits methyltransferase activity by interacting with the SET domain of EZH2^[1]. (Pink: EZH2 ligand (HY-147230); Blue: Cereblon ligand (HY-103596); Black: linker).

EZH2 is a histone methyltransferase and the catalytic subunit of Polycomb Repressive Complex 2 (PRC2). It plays a pivotal role in tumor epigenetics by transcriptionally repressing tumor suppressor genes. As an epigenetic enzyme that exerts core regulatory functions in tumorigenesis and progression, EZH2 serves as both a target for existing therapies and a key research subject for the next-generation protein degradation technology (PROTACs)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

928.13

C₅₃H₆₅N₇O₈

2653338-70-4

CCN(C1CCOCC1)C2=CC(C3=CC=C(C=C3)CN4CCN(CC4)CCCCCCOC5=C(C6=CC=C5)C(N(C6=O)C7CCC(NC7=O)=O)=O)=CC(C(NCC8=C(C=C(NC8=O)C)C)=O)=C2C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. S Abulkhair H, et al. Therapeutic horizons in the development of PROTAC-based EZH2 inhibitors: recent achievements, comparative analysis, and future perspectives. RSC Adv. 2026;16(4):3034-3056. Published 2026 Jan 14.  [Content Brief]