2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase

Histone Methyltransferase

Histone Methyltransferase

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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 Isoform Specific Products:

Histone Methyltransferase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-155050
    PRMT5-IN-31
    		Inhibitor 99.25%
    PRMT5-IN-31 (Compound 3m) is a selective PRMT5 inhibitor (IC50: 0.31 μM). PRMT5-IN-31 up-regulates hnRNP E1 protein level. PRMT5-IN-31 occupies the substrate site of PRMT5 and forms essential interactions with amino acid residues. PRMT5-IN-31 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. PRMT5-IN-31 has high metabolic stability on human liver microsomes (T1/2: 132.4 min).
    PRMT5-IN-31
  • HY-15214A
    CARM1-IN-3 dihydrochloride
    		Inhibitor 98.77%
    CARM1-IN-3 dihydrochloride (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively.
    CARM1-IN-3 dihydrochloride
  • HY-181789
    DOT1L808
    		Degrader
    DOT1L808 is a potent and highly selective DOT1L PROTAC degrader with a DC50 value of 5 nM. DOT1L808 can promote the ubiquitination and degradation of DOT1L. DOT1L808 exhibits antitumor activity in an orthotopic leukemia model.
    DOT1L808
  • HY-173561
    MS115
    		Inhibitor
    MS115 is a selective PRMT5/MEP50 PROTAC degrader, with DC50 values of 17.4 nM and 11.3 nM for PRMT5 and MEP50, respectively. MS115 promotes PRMT5/MEP50 ubiquitination and degradation. MS115 shows anticancer activity against breast cancer.
    MS115
  • HY-178321
    UNC10088
    		Degrader
    UNC10088 is a molecular glue targeting NSD2. UNC10088 mediates the formation of a stable ternary complex between SCFFBXO22 and the NSD2 PWWP1 domain. UNC10088 promotes ubiquitination of the SCFFBXO22-dependent NSD2 PWWP1 domain through reversible covalent bonding with the C326 region of FBXO22. UNC10088 could be used in cancer research.
    UNC10088
  • HY-168992
    UNC6535
    		Inhibitor
    UNC6535 is a covalent ligand targeting the SETDB1 triple Tudor domain (3TD) with negative allosteric modulator properties, with an IC50 of 3.4 μM and a Kd of 4.2 μM. UNC6535 inhibits the methyltransferase activity of recombinant SETDB1 protein lacking the 3TD domain. UNC6535 reversibly binds to the aromatic cages of both TD2 and TD3 subdomains of SETDB1 3TD simultaneously, displacing the endogenous H3K9Me2K14Ac histone tail ligand. UNC6535 can be used in research on cancer and neurodegenerative diseases.
    UNC6535
  • HY-177499
    NSD2-IN-5
    		Inhibitor
    NSD2-IN-5 (Compound 198) is an NSD2 inhibitor with an IC50 value between 0.001 μM and 0.01 μM. NSD2-IN-5 can be used in cancer research.
    NSD2-IN-5
  • HY-163561A
    CARM1-IN-6 dihydrochloride
    		Inhibitor 98.44%
    CARM1-IN-6 (Compound iCARM1) dihydrochloride is an effective and selective inhibitor of CARM1 with an IC50 value of 12.3 μM. CARM1-IN-6 dihydrochloride exhibits cell growth inhibitory activity and can be used in cancer research.
    CARM1-IN-6 dihydrochloride
  • HY-116971
    DCG066
    		Inhibitor 99.78%
    DCG066 is an inhibitor of lysine methyltransferase G9a. DCG066 can bind directly to G9a and inhibit methyltransferase activity in vitro. DCG066 decreases di-methylation levels of histone H3 lysine 9 (H3K9Me2), inhibits cell proliferation and induces cell apoptosis. DCG066 displays low cytotoxicity in leukemia cell lines with high levels of G9a expression, including K562.
    DCG066
  • 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.
    Dot1L-IN-2
  • HY-144882
    (R)-HH2853
    		Inhibitor
    (R)-HH2853 is a mutant EZH2 inhibitor with an IC50 of <100 nM for EZH2-Y641F. (R)-HH2853 can be used for cancer and autoimmune diseases (WO2018045971A1; compound 201).
    (R)-HH2853
  • HY-44062
    G9a-IN-1
    		Inhibitor 98.12%
    G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer.
    G9a-IN-1
  • HY-B1226
    Diperodon hydrochloride
    		Inhibitor 98.46%
    Diperodon hydrochloride exerts its effect by being broken down by serum degradoses.
    Diperodon hydrochloride
  • HY-12335A
    UNC0379 TFA
    		Inhibitor 99.91%
    UNC0379 TFA 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 TFA can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma.
    UNC0379 TFA
  • HY-134883
    PRMT5-IN-4
    		Inhibitor 99.0%
    PRMT5-IN-4 is a PRMT5 inhibitor. PRMT5-IN-4 is applicable for cancer research.
    PRMT5-IN-4
  • HY-W025074
    BML-278
    		98.49%
    BML-278 is a SIRT1 activator (EC150: 1 μM). BML-278 increases H3K9 methylation and inhibits H3K9 acetylation in both the paternal and maternal pronucleus. BML-278 improves early embryonic development. BML-278 arrests the cell cycle at the G1/S phase, and reduces senescence in primary human mesenchymal cells. BML-278 reduces tubulin acetylation in U937 cells. BML-278 also increases mitochondrial density in murine C2C12 myoblasts.
    BML-278
  • HY-103663A
    MAK683 hydrochloride
    		Inhibitor
    MAK683 hydrochloride is an embryonic ectoderm development (EED) inhibitor extracted from patent US20160176882 A1, compound example 2. MAK683 exhibits IC50s of 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay.
    MAK683 hydrochloride
  • HY-142211
    PRMT5-IN-15
    		Inhibitor
    PRMT5-IN-15 is a PRMT5 inhibitor with an IC50 value of 0.84 nM.
    PRMT5-IN-15
  • HY-100855
    DC_C66
    		Inhibitor
    DC_C66 is a cell-permeable, selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 1.8 μM. DC_C66 has a good selectivity for CARM1 against PRMT1 (IC50=21 μM), PRMT6 (IC50= 47μM), and PRMT5.
    DC_C66
  • HY-10587A
    BIX-01294 hydrochloride hydrate
    		Inhibitor
    BIX-01294 hydrochloride hydrate is a histone-lysine methyltransferase (HMTase) inhibitor, which selective inhibits the G9aHMTase with IC50 of 1.7 μM, reduces histone-3 lysine (9) methylation (H3K9me), induces autophagy and apoptosis in human glioma cells.
    BIX-01294 hydrochloride hydrate
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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