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 (71):

Cat. No. Product Name Effect Purity
  • HY-13470
    GSK126 Inhibitor 99.86%
    GSK126 is a potent, highly selective inhibitor of EZH2 methyltransferase activity with IC50 of 9.9 nM.
  • HY-13803
    EPZ-6438 Inhibitor 99.63%
    EPZ-6438 inhibits the activity of human PRC2-containing wild-type EZH2 with Ki of 2.5±0.5 nM.
  • HY-13980
    UNC0642 Inhibitor 99.81%
    UNC0642 is a potent and selective G9a/GLP inhibitor, inhibits G9a/GLP with an IC50 of less than 2.5 nM.
  • HY-13500
    GSK343 Inhibitor 98.49%
    GSK343 is a highly potent, selective, and cell-active EZH2 inhibitor with IC50 of 4 nM.
  • HY-12186
    3-Deazaneplanocin A hydrochloride Inhibitor 99.76%
    3-Deazaneplanocin A hydrochloride is a potent histone methyltransferase EZH2 inhibitor.
  • HY-19563
    A-893 Inhibitor
    A-893 is a cell-active inhibitor of Methyltransferase SMYD2, with an IC50 of 2.8 nM.
  • HY-111390
    Dot1L-IN-2 Inhibitor
    Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively.
  • HY-12991A
    BIX-01338 hydrate Inhibitor
    BIX-01338 hydrate is a histone lysine methyltransferase inhibitor.
  • HY-15593
    EPZ-5676 Inhibitor 99.75%
    EPZ-5676 is a potent and selective aminonucleoside inhibitor of DOT1L histone methyltransferase with Ki of < 80 pM, demonstrating > 37,000-fold selectivity against all other PMTs tested, and inhibits H3K79 methylation in tumor.
  • HY-19324
    EPZ031686 Inhibitor 99.63%
    EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 and 1.1 nM respectively.
  • HY-15646
    UNC1999 Inhibitor 99.47%
    UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH2 (IC50<10 nM) and EZH1 (IC50=45±3 nM).
  • HY-15226A
    AZ505 ditrifluoroacetate Inhibitor 99.99%
    AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.
  • HY-12727
    EPZ015666 Inhibitor 98.56%
    EPZ015666 is an orally available inhibitor of PRMT5 enzymatic activity in biochemical assays with IC50 of 22 nM and broad selectivity against a panel of other histone methyltransferases.
  • HY-19313
    LLY-507 Inhibitor 99.09%
    LLY-507 is a potent inhibitor of SMYD2 with IC50 < 15 nM, is >100-fold selective for SMYD2 over a broad range of methyltransferase and non-methyltransferase targets.
  • HY-15227
    EPZ004777 Inhibitor 99.89%
    EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
  • HY-101563
    GSK3326595 Inhibitor 99.24%
    GSK3326595 is a potent, selective, reversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with broad anti-proliferative activity.
  • HY-19615
    MS023 Inhibitor 99.84%
    MS023 is a potent, selective, and cell-active inhibitor of human type I PRMTs with IC50 of 4-119 nM.
  • HY-15273
    UNC0638 Inhibitor 99.87%
    UNC0638 is a potent G9a (EHMT2) (IC50<15 nM) and GLP (EHMT1) inhibitor (IC50=19 nM) in S-adenosyl-L-homocysteine hydrolase (SAHH)-coupled assays.
  • HY-100235
    EPZ015866 Inhibitor 98.71%
    EPZ015866 (GSK591) is a potent selective inhibitor of the arginine methyltransferase PRMT5. It maintained excellent selectivity against other PMT enzymes observed with EPZ015666 [1].
  • HY-12583
    A-366 Inhibitor 98.47%
    A-366 is a peptide-competitive inhibitor of G9a/GLP with an enzymatic IC50 of ~3 nM and >100-fold selectivity over other methyltransferases and other non-epigenetic targets.
Isoform Specific Products

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