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-163588
    GTA182
    		Inhibitor 99.60%
    GTA182 (compound 107) is an orally active PRMT5 inhibitor and can be used for study of cancer.
    GTA182
  • HY-161759
    MS152
    		Inhibitor 99.36%
    MS152 is an oral bioactive inhibitor of EHMT2/G9a. MS152 reactivats maternally silenced Prader-Willi syndrome (PWS) genes in brain and liver tissues of PWS mouse models.
    MS152
  • HY-134828
    AZ506
    		Inhibitor 99.74%
    AZ506 is a potent SMYD2 inhibitor with an IC50 of 17 nM. AZ506 inhibits SMYD2 methyltransferase activity in cells, leading to a decrease in the SMYD2-mediated methylation signal.
    AZ506
  • HY-171119
    NSD2-PWWP1-IN-1
    		Inhibitor 98.72%
    NSD2-PWWP1-IN-1 (compound 31) is a potent NSD2-PWWP1 inhibitor with an IC50 value of 0.64 µM. NSD2-PWWP1-IN-1 has the potential for the research of cancer.
    NSD2-PWWP1-IN-1
  • HY-162749A
    G9D-4 TFA
    		Degrader 99.44%
    G9D-4 TFA is a G9a PROTAC degrader. G9D-4 TFA induces G9a degradation, reduces H3K9me2 levels, and prevents GLP interference via the CRBN ternary complex, proteasome and ubiquitin-like modification-dependent pathways. G9D-4 TFA exerts antiproliferative activity and induces Apoptosis in pancreatic cancer cells. G9D-4 TFA can be used for research on pancreatic cancer.
    G9D-4 TFA
  • HY-139611B
    (S)-Navlimetostat
    		Inhibitor 98.15%
    (S)-Navlimetostat (example 16-7) is the S-enantiomer of Navlimetostat. (S)-Navlimetostat is a PRMT5/MTA complex inhibitor, with an IC50 of 7070 nM.
    (S)-Navlimetostat
  • HY-151576
    PRMT5:MEP50 PPI
    		Inhibitor 98.09%
    PRMT5:MEP50 PPI is a novel PRMT5:MEP50 protein-protein interaction (PRMT5:MEP50 PPI) inhibitor, shows anti-tumor activity and anti-proliferative activity of lung and prostate cancer cells.
    PRMT5:MEP50 PPI
  • HY-12991A
    BIX-01338 hydrate
    		Inhibitor 98.67%
    BIX-01338 hydrate is a histone lysine methyltransferase inhibitor.
    BIX-01338 hydrate
  • HY-126300
    SGC6870
    		Inhibitor 99.80%
    SGC6870, a chemical probe, is a potent, selective and cytoactive allosteric inhibitor of PRMT6 with IC50 of 77 nM.
    SGC6870
  • HY-128352
    SMYD3-IN-1
    		Inhibitor 98.03%
    SMYD3-IN-1 (compound 29) is an irreversible and selective inhibitor of SMYD3 (SET and MYND domain containing 3), with an IC50 of 11.7 nM.
    SMYD3-IN-1
  • HY-111904
    EHMT2-IN-2
    		Inhibitor 99.0%
    EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disease or cancer.
    EHMT2-IN-2
  • HY-141877B
    MS4322 (isomer)
    		99.87%
    MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )).
    MS4322 (isomer)
  • HY-132970
    EED ligand 1
    		Inhibitor 99.93%
    EED ligand 1 is a diverse, potent, and efficacious inhibitor that target the EED subunit of the polycomb repressive complex 2 (PRC2) methyltransferase.
    EED ligand 1
  • HY-120444
    MS0124
    		Inhibitor 99.79%
    MS0124 is a potent selective G9a-like protein (GLP) inhibitor with IC50 values of 13±4 nM and 440±63 nM for GLP and G9a,respectively.
    MS0124
  • HY-147185
    PRMT7-IN-1
    		Inhibitor 98.70%
    PRMT7-IN-1 (Compound 14) is a PRMT7 inhibitor with an IC50 of 2.1 μM. PRMT7-IN-1 shows anticancer activity against different cancer cells.
    PRMT7-IN-1
  • HY-147230
    EZH2-IN-13
    		Inhibitor 99.72%
    EZH2-IN-13 is a potent EZH2 inhibitor, for details please refer to compound 73 in patent WO2017139404. EZH2-IN-13 can be used to study cancers or precancerous lesions associated with EZH2 activity.
    EZH2-IN-13
  • HY-171120
    NSD2-PWWP1-IN-2
    		Inhibitor 99.64%
    NSD2-PWWP1-IN-2 (compound 33) is a potent NSD2-PWWP1 inhibitor with an IC50 value of 1.49 µM. NSD2-PWWP1-IN-2 has the potential for the research of cancer.
    NSD2-PWWP1-IN-2
  • HY-100967
    SKF 91488 dihydrochloride
    		Inhibitor 98.62%
    SKF 91488 (Homodimaprit) dihydrochloride is a potent and noncompetitive histamine N-methyltransferase inhibitor with a Ki value of 0.9 μM. SKF 91488 dihydrochloride can block histamine metabolism and increase histamine concentrations. SKF 91488 dihydrochloride can increase blood pressure and enhance bronchoconstriction. SKF 91488 can be used for the researches of infection, inflammation and cardiovascular disease, such as Mycoplasma pneumonia and hemorrhagic hypotension.
    SKF 91488 dihydrochloride
  • HY-160801
    HKYK-0030
    		Inhibitor 99.38%
    HKYK-0030 is an inhibitor for MTDH-SND1 protein-protein interaction. HKYK-0030 exhibits inhibitory activity against cancer metastasis.
    HKYK-0030
  • HY-171121
    NSD2-PWWP1-IN-3
    		Inhibitor 99.63%
    NSD2-PWWP1-IN-3 (compound 36) is a potent NSD2-PWWP1 inhibitor with an IC50 value of 8.05 µM. NSD2-PWWP1-IN-3 has the potential for the research of cancer.
    NSD2-PWWP1-IN-3
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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