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 (60):

Cat. No. Product Name Effect Purity
  • 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-13470
    GSK126 Inhibitor 99.32%
    GSK126 is a potent, highly selective inhibitor of EZH2 methyltransferase activity with IC50 of 9.9 nM.
  • HY-13500
    GSK343 Inhibitor 99.58%
    GSK343 is a highly potent, selective, and cell-active EZH2 inhibitor with IC50 of 4 nM.
  • HY-12186
    3-Deazaneplanocin A hydrochloride Inhibitor
    3-Deazaneplanocin A hydrochloride is a potent histone methyltransferase EZH2 inhibitor.
  • 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-100565
    SGC2085 Inhibitor 99.10%
    SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 50 nM.
  • HY-19809
    MI-463 Inhibitor 99.46%
    MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.
  • HY-101563
    GSK3326595 Inhibitor 99.24%
    GSK3326595 is a PRMT5 inhibitor extracted from patent WO 2016022605 A1, Formula A.
  • 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-10587
    BIX-01294 Inhibitor 99.22%
    BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM.
  • HY-15227
    EPZ004777 Inhibitor 99.89%
    EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
  • HY-15646
    UNC1999 Inhibitor 99.02%
    UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH2 (IC50<10 nM) and EZH1 (IC50=45±3 nM).
  • HY-15273
    UNC0638 Inhibitor 98.60%
    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-19324
    EPZ031686 Inhibitor 99.60%
    EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 and 1.1 nM respectively.
  • HY-18627A
    PFI-2 hydrochloride Inhibitor 98.60%
    PFI-2 hydrochloride is a a first-in-class, potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 with IC50 of 2 nM, 500 fold active than (S)-PFI-2.
  • 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-15650
    SGC0946 Inhibitor 99.75%
    SGC0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM; selectively kill mixed lineage leukaemia cells.
  • HY-15226A
    AZ505 ditrifluoroacetate Inhibitor 99.50%
    AZ505 ditrifluoroacetate is a potent and highly selective inhibitor of the oncogenic protein SMYD2(IC50=0.12 uM) with potential anticancer activity, >600 fold than SMYD3(IC50>83.3 uM); DOT1L(IC50>83.3 uM);EZH2(IC50>83.3 uM).
  • HY-12583
    A-366 Inhibitor 98.83%
    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.
  • HY-12856
    GSK503 Inhibitor 99.29%
    GSK503 is a potent and specific inhibitor of EZH2 methyltransferase with Kiapp values of 3 to 27 nM.