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EZH2 inhibitors

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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
Verified customer review of EPZ-6438 (Tazemetostat)
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 tumor 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
Verified customer review of GSK126
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 analog 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
Verified customer review of 3-Deazaneplanocin A (DZNep) Hydrochloride
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 methyltransferases. GSK343 induces autophagy.
Cell, 2025, S0092-8674(25)00396-4
Research (Wash D C), 2025, 8:0602
Mol Genet Genomics, 2025, 300(1):63
Verified customer review of GSK343
E1521New SHR2554 SHR2554 is an inhibitor of EZH2. SHR2554 exhibits anti-tumor activity with IC50 values ranging from 0.365 to 3.001 μM 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.
E4850 Tazemetostat hydrobromide Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective, and orally available inhibitor of EZH2. It inhibits EZH2 with IC50 values of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide also inhibits EZH1 with an IC50 of 392 nM.