1. Epigenetics
  2. 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.

Histone Methyltransferase Related Products (76):

Cat. No. Product Name Effect Purity
  • HY-13470
    GSK126 Inhibitor 99.98%
    GSK126 is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC50 of 9.9 nM.
  • HY-13803
    Tazemetostat Inhibitor 99.76%
    Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor with Ki and IC50 of 2.5 and 11 nM, respectively.
  • HY-13500
    GSK343 Inhibitor 98.49%
    GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.
  • HY-13980
    UNC0642 Inhibitor 99.81%
    UNC0642 is a potent and selective G9a/GLP inhibitor, with an IC50 of less than 2.5 nM.
  • HY-12186
    3-Deazaneplanocin A hydrochloride Inhibitor 99.76%
    3-Deazaneplanocin A hydrochloride is a potent histone methyltransferase EZH2 inhibitor.
  • HY-117421
    CM-579 Inhibitor
    CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells.
  • HY-101520
    Dot1L-IN-1 Inhibitor
    Dot1L-IN-1 is a highly potent, selective and structurally novel Dot1L inhibitor with a Ki of 2 pM.
  • HY-111544
    EML741 Inhibitor
    EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated.
  • HY-15593
    Pinometostat Inhibitor 99.92%
    Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.
  • HY-101563
    GSK3326595 Inhibitor 99.24%
    GSK3326595 is a potent, selective, reversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC50 of 6.2 nM.
  • HY-10587
    BIX-01294 Inhibitor 98.61%
    BIX-01294 is an inhibitor of G9a Histone Methyltransferase with IC50 of 1.9 μM.
  • HY-15646
    UNC1999 Inhibitor 99.47%
    UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH1/2 with IC50s of 10 nM and 45 nM, repectively.
  • HY-15226A
    AZ505 ditrifluoroacetate Inhibitor 99.99%
    AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.
  • HY-15227
    EPZ004777 Inhibitor 99.89%
    EPZ004777 is a potent, selective DOT1L inhibitor with an IC50 of 0.4 nM.
  • HY-101117
    EED226 Inhibitor 98.70%
    EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.
  • HY-19615
    MS023 Inhibitor 99.50%
    MS023 is a potent and cell-permeable protein arginine methyltransferases (PRMTs) inhibitor with IC50s of 20, 119, 83, 8, and 8 nM for PRMT1, 3, 4, 6, and 8.
  • HY-N2019
    Chaetocin Inhibitor >98.0%
    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.
  • HY-15650
    SGC0946 Inhibitor 98.48%
    SGC0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM; selectively kill mixed lineage leukaemia cells.
  • HY-19324
    EPZ031686 Inhibitor 99.63%
    EPZ031686 is an orally available SMYD3 inhibitor with an IC50 of 3 nM in cell-free assay.
  • HY-100235
    EPZ015866 Inhibitor 99.98%
    EPZ015866 is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 22 nM.
Isoform Specific Products

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