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Histone Methyltransferase inhibitors

Other Epigenetics Related Inhibitors

BET DNA Methyltransferase p300/CBP Histone Demethylase Histone Acetyltransferase MicroRNA NSD EZH1 RNA Methyltransferase SF3B

Isoform-selective Products

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)
S8664 GSK3326595 (Pemrametostat, EPZ015938) Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models.
MedComm (2020), 2025, 6(6):e70150
J Med Chem, 2025, 68(4):4217-4236
J Med Chem, 2025, 68(5):5097-5119
S7062 Pinometostat (EPZ5676) Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM in a cell-free assay, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1.
Nat Commun, 2025, 16(1):10324
Blood Adv, 2025, bloodadvances.2024015427
J Neurotrauma, 2025, 10.1177/08977151251374286
Verified customer review of Pinometostat (EPZ5676)
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
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
S8006 BIX-01294 trihydrochloride BIX-01294 trihydrochloride is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3.
Clin Transl Med, 2025, 15(1):e70164
Mol Metab, 2025, 94:102113
Acta Pharm Sin B, 2024, 14(3):1187-1203
Verified customer review of BIX-01294 trihydrochloride
S7165 UNC1999 UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets. This compound is a potent autophagy inducer. It specifically suppresses H3K27me3/2 and induces a range of anti-leukemia effects including anti-proliferation, differentiation, and apoptosis.
Cell Stem Cell, 2025, S1934-5909(25)00041-4
Cell Rep, 2025, 44(5):115673
bioRxiv, 2025, 2025.05.22.655558
Verified customer review of UNC1999
S7748 EPZ015666 (GSK3235025) EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.
MedComm (2020), 2025, 6(6):e70150
Cell Rep, 2024, 43(11):114930
Oncogene, 2024, 10.1038/s41388-024-03049-6
Verified customer review of EPZ015666 (GSK3235025)
S7353 EPZ004777 EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM in a cell-free assay and demonstrates >1,200-fold selectivity for DOT1L over all other tested PMTs. EPZ004777 induces apoptosis.
NPJ Regen Med, 2024, 9(1):42
Cell Rep, 2023, 42(8):112885
Cell Rep, 2023, 42(6):112566
Verified customer review of EPZ004777
S7265 MM-102 (HMTase Inhibitor IX) MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic inhibitor of the WDR5/MLL1 protein-protein interaction, which bind to WDR5 with Ki < 1 nM and IC50 =2.4nM.This product may precipitate when dissolved in saline solution or PBS solution. It is recommended to prepare the stock solution in DMSO solution.
Nat Commun, 2025, 16(1):5222
Nat Commun, 2025, 16(1):7483
Cell Rep Med, 2025, 6(2):101928
Verified customer review of MM-102 (HMTase Inhibitor IX)

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