1. Signaling Pathways
  2. Epigenetics
  3. Histone Methyltransferase

Histone Methyltransferase

Histone modifications play critical roles in regulating both global and stage-specific gene expression. Methylation on histones H3K4, H3K36 and H3K79 is generally associated with gene activation, whereas methylation on histones H3K9 and H3K27 is generally associated with gene repression. Histone lysine methylation is dynamically regulated by site-specific methyltransferases and demethylases. EZH2 (the catalytic subunit of PRC2) is responsible for the methylation of H3K27 in cells.

DOT1L is a histone H3 lysine 79 methyltransferase whose inhibition increases the yield of induced pluripotent stem cells (iPSCs). EPZ-5676 is a potent and selective DOT1L inhibitor.

Crucial to PRC2 activity, the histone methyltransferase enhancer of zeste homolog 2 (EZH2) tri-methylates lysine 27 of histone 3 (H3K27me3), leading to chromatin condensation and transcriptional repression.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13470
    GSK126
    Inhibitor 99.98%
    GSK126 (GSK2816126A) is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC50 of 9.9 nM.
    GSK126
  • HY-15593
    Pinometostat
    Inhibitor 99.99%
    Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.
    Pinometostat
  • HY-13803
    Tazemetostat
    Inhibitor 99.93%
    Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells.
    Tazemetostat
  • HY-101563
    GSK3326595
    Inhibitor 99.97%
    GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma.
    GSK3326595
  • HY-12186
    3-Deazaneplanocin A hydrochloride
    Inhibitor 99.98%
    3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A hydrochloride also has anti-orthopoxvirus and anti-variola activities.
    3-Deazaneplanocin A hydrochloride
  • HY-150190
    F5446
    99.38%
    F5446 (compound 1) is an inhibitor of SUV39H1 methyltransferase. F5446 induces human colon carcinoma cell death in a dose-dependent manner.
    F5446
  • HY-157251
    UNC8153 TFA
    Inhibitor 99.91%
    UNC8153 TFA is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 TFA reduces the cellular levels of both NSD2 protein and the H3K36me2 chromatin mark. UNC8153 TFA contains a simple warhead that confers proteasome-dependent degradation of NSD2.
    UNC8153 TFA
  • HY-13500
    GSK343
    Inhibitor 99.88%
    GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.
    GSK343
  • HY-12727
    EPZ015666
    Inhibitor 99.83%
    EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 with an IC50 of 22 nM.
    EPZ015666
  • HY-136328
    EZM0414 TFA
    Inhibitor 99.42%
    EZM0414 TFA is a potent, selective and orally active inhibitor of SETD2 which is a human histone methyltransferase. EZM0414 TFA has anti-proliferative effects.
    EZM0414 TFA
  • HY-10587
    BIX-01294
    Inhibitor 98.75%
    BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells.
    BIX-01294
  • HY-128717A
    GSK3368715 dihydrochloride
    Inhibitor 99.94%
    GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.
    GSK3368715 dihydrochloride
  • HY-101117
    EED226
    Inhibitor 99.65%
    EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model. EED226 is a potent, selective, and orally bioavailable EED inhibitor. EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays.
    EED226
  • HY-N2019
    Chaetocin
    Inhibitor 99.46%
    Chaetocin is a specific inhibitor of the histone methyltransferase (HMT) SU(VAR)3-9 with an IC50 of 0.6 μM for SU(VAR)3-9. It also inhibits thioredoxin reductase (TrxR) with an IC50 of 4 μM.
    Chaetocin
  • HY-101564
    Onametostat
    Inhibitor 99.79%
    Onametostat (JNJ-64619178) is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.14 nM. Onametostat has potent activity in lung cancer.
    Onametostat
  • HY-19615
    MS023
    Inhibitor 99.73%
    MS023 is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
    MS023
  • HY-15646
    UNC1999
    Inhibitor 99.83%
    UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH2/1 with IC50s of <10 nM and 45 nM, repectively.
    UNC1999
  • HY-12335
    UNC0379
    Inhibitor 99.90%
    UNC0379 is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM, KD value of 18.3 μM. UNC0379 can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma.
    UNC0379
  • HY-111109
    EZM 2302
    Inhibitor 99.59%
    EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1) with an IC50 of 6 nM.
    EZM 2302
  • HY-10929
    UNC0224
    Inhibitor 99.31%
    UNC0224 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 2.6 nM, an IC50 of 15 nM and a Kd of 23 nM. UNC0224 also potently inhibits b>GLP with assay-dependent IC50 values of 20-58 nM. UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E.
    UNC0224
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