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EZH2 Inhibitors

Other Methylation Related 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, nan
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
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.
Science Advances, 2024, eadk4423
Sci Adv, 2024, 10(13):eadk4423
JCI Insight, 2022, e155899
S7616 CPI-169 CPI-169 is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.
J Exp Clin Cancer Res, 2023, 42(1):96
Nat Commun, 2022, 13(1):6226
Cell Chem Biol, 2021, S2451-9456(21)00213-0
S8918 MS1943 MS1943 is an orally bioavailable EZH2 selective degrader that effectively reduces EZH2 levels in cells with IC50 of 120 nM for inhibiting EZH2 methyltransferase activity.
Nat Commun, 2024, 15(1):9755