EZH2 inhibitors

Other Methylation Inhibitors

• Featured Inhibitors
• Inhibitors (23)
• Chemical (1)

Cat.No.	Product Name	Information	Product Use Citations	Product Validations
S7128	EPZ-6438 (Tazemetostat)	Tazemetostat (EPZ-6438, E7438) is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.	Nat Cancer, 2025, 10.1038/s43018-025-00960-z Nat Cell Biol, 2025, 27(9):1411-1421 Nat Commun, 2025, 16(1):10324
S9655	PF-06821497	PF-06821497 is a selective and orally active inhibitor of Zeste Homolog 2 (EZH2) with a Ki value <0.1 nM against mutant Y641N EZH2. It exhibits robust tumour growth inhibition.
S7061	GSK126	GSK126 (GSK2816126A, GSK2816126) is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases.	Theranostics, 2025, 15(14):7127-7153 EMBO J, 2025, 10.1038/s44318-025-00537-7 EBioMedicine, 2025, 119:105879
E1497	Tulmimetostat (CPI-0209)	Tulmimetostat (CPI-0209) is an orally bioavailable and selective inhibitor of EZH2 that has therapeutic potential for androgen receptor-dependent prostate cancer.	bioRxiv, 2025, 2025.07.07.663486
S8926	Valemetostat (DS-3201)	Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor.	Cell Rep Med, 2025, S2666-3791(25)00102-8 Genes Dev, 2025, 10.1101/gad.353002.125 NPJ Precis Oncol, 2025, 9(1):69
S7120	3-Deazaneplanocin A (DZNep) Hydrochloride	DZNep (3-deazaneplanocin A) HCl, an analogue of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM in a cell-free assay.	Nat Cell Biol, 2025, 27(7):1175-1185 Genes Dev, 2025, 39(3-4):280-298 Cell Biosci, 2025, 15(1):146
S7164	GSK343	GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other Histone Methyltransferase. GSK343 induces Autophagy.	Cell, 2025, S0092-8674(25)00396-4 Research (Wash D C), 2025, 8:0602 Mol Genet Genomics, 2025, 300(1):63
S8353	Lirametostat (CPI-1205)	Lirametostat (CPI-1205) is an orally available selective inhibitor of the histone lysine methyltransferase EZH2 with IC50 values of 2 nM and 52 nM for EZH2 and EZH1 respectively. It has potential antineoplastic activity.	Sci Adv, 2024, 10(13):eadk4423 JCI Insight, 2022, e155899 Cancer Discov, 2021, candisc.0913.2020
E1521New	SHR2554	SHR2554 is an inhibitor of EZH2. SHR2554 exhibits anti-tumour activity with IC50 values ranging from 0.365 to 3.001 M in a dose-dependent manner, in T-cell lymphoma (TCL) by reducing H3K27me3 levels.
E4678New	EZH2/HSP90-IN-29	EZH2/HSP90-IN-29 is a potent dual inhibitor of EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively, that induces M-phase cell cycle arrest, promotes apoptosis/necrosis-related gene expression, and inhibits ROS catabolism. It crosses the blood-brain barrier and can show potential as a tractable anti-GBM agent for glioblastoma research.
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