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 (59):

Cat. No. Product Name Effect Purity
  • HY-13803
    EPZ-6438 Inhibitor
    EPZ-6438 inhibits the activity of human PRC2-containing wild-type EZH2 with Ki of 2.5±0.5 nM.
  • HY-13470
    GSK126 Inhibitor
    GSK126 is a potent, highly selective inhibitor of EZH2 methyltransferase activity with IC50 of 9.9 nM.
  • HY-13500
    GSK343 Inhibitor
    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-15593
    EPZ-5676 Inhibitor
    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-15273
    UNC0638 Inhibitor
    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-15227
    EPZ004777 Inhibitor
    EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
  • HY-10587
    BIX-01294 Inhibitor
    BIX-01294 is an inhibitor of G9a Histone Methyltransferase with IC50 of 1.9 μM.
  • HY-15646
    UNC1999 Inhibitor
    UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH2 (IC50<10 nM) and EZH1 (IC50=45±3 nM).
  • HY-15555
    EPZ005687 Inhibitor
    EPZ005687 is a potent and selective inhibitor of Epigenetic Reader Domain with Ki of 24 nM, and has 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
  • HY-15650
    SGC0946 Inhibitor
    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
    AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.
  • HY-15573
    EI1 Inhibitor
    EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
  • HY-15222
    MI-2 Inhibitor
    MI-2 is a Menin-MLL interaction inhibitor with IC50 of 446±28 nM.
  • HY-15226
    AZ505 Inhibitor
    AZ505 is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.
  • HY-15649
    UNC1215 Antagonist
    UNC1215 is a potent and selective chemical probe for the methyllysine (Kme) reading function of L3MBTL3 with Kd value of 120 nM.
  • HY-13808
    UNC 0631 Inhibitor
    UNC 0631 is a potent G9a inhibitor with IC50 value of 4 nM.
  • HY-10930
    UNC0321 Inhibitor
    UNC0321 is a potent and selective G9a inhibitor with Ki of 63 pM, UNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date.
  • HY-15223
    MI-3 Inhibitor
    MI-3 is a Menin-MLL interaction inhibitor with IC50 value of 648 ± 25 nM.
  • HY-15647
    BRD9539 Inhibitor
    BRD9539 inhibits G9a activity with an IC50 of 6.3 μM, inhibits PRC2 activity with a similar IC50.