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  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. Nom du produit Effet Pureté Chemical Structure
  • HY-152775
    RK-701
    		Inhibitor 98.01%
    RK-701 is an highly selective and non-genotoxic inhibitor of G9a with IC50 value of 23-27 nM. RK-701 selectively up-regulates HbF, γ- Globin, BGLT3 expression, down-regulates H3K9me2 expression. RK-701 also has inhibition for BCL11A and ZBTB7A.
    RK-701
  • HY-103682
    PF-06726304
    		Inhibitor 99.71%
    PF-06726304 is a potent and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 displays robust antitumor growth activity.
    PF-06726304
  • HY-19324
    EPZ031686
    		Inhibitor 99.71%
    EPZ031686 is an potent and orally active SMYD3 inhibitor and with an IC50 value of 3 nM. EPZ031686 can be used for cancer research.
    EPZ031686
  • HY-N5024
    Gambogenic acid
    		Inhibitor 99.91%
    Gambogenic acid is an active ingredient that can be isolated from gamboge. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination. Gambogenic acid can be used for the research of cancer.
    Gambogenic acid
  • HY-16986
    EPZ011989
    		Inhibitor 98.79%
    EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ011989 shows robust methyl mark inhibition and anti-tumor activity. EPZ011989 can be used for the research of various cancers. EPZ011989 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    EPZ011989
  • HY-19615B
    MS023 dihydrochloride
    		Inhibitor 99.68%
    MS023 dihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
    MS023 dihydrochloride
  • HY-148334
    MS8815
    		Inhibitor 99.95%
    MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader. MS8815 has inhibition activity for EZH2 with an IC50 value of 8.6 nM. MS8815 can be used for the research of triple-negative breast cancer (TNBC).
    MS8815
  • HY-19546
    BAY-598
    		Inhibitor 99.33%
    BAY-598, a chemical probe, is selective small molecule inhibitor of SMYD2 with an IC50 of 27 nM.
    BAY-598
  • HY-21972
    BCI-121
    		Inhibitor 99.89%
    BCI-121 is a SMYD3 inhibitor that impairs the proliferation of cancer cell.
    BCI-121
  • HY-100625
    BVT948
    		Inhibitor ≥99.0%
    BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8 (KMT5A).
    BVT948
  • HY-122181B
    OTS186935 hydrochloride
    		Inhibitor 99.58%
    OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells.
    OTS186935 hydrochloride
  • HY-15555
    EPZ005687
    		Inhibitor 99.46%
    EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, and has 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
    EPZ005687
  • HY-119344
    MS37452
    		Inhibitor 99.81%
    MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a Kd of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells.
    MS37452
  • HY-134086
    NSD-IN-2
    		Inhibitor 98.16%
    NSD-IN-2 is a potent and irreversible NSD inhibitor with inhibitory activity towards members of the NSD family (NSD1/2/3). NSD-IN-2 can be used in research of acute myeloid leukemia.
    NSD-IN-2
  • HY-132922
    EEDi-5273
    		Inhibitor 99.48%
    EEDi-5273 (APG-5918) is a potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 of 0.2 nM. EEDi-5273 can inhibit the polycomb repressive complex 2 (PRC2) activity and block trimethylation of histone H3 lysine 27. EEDi-5273 can be used for the research of cancer, such as ovarian cancer.
    EEDi-5273
  • HY-114209
    MRK-740
    		Inhibitor 99.13%
    MRK-740, a chemical probe, is a potent, selective and substrate-competitive PRDM9 histone methyltransferase inhibitor with an IC50 of 80?nM. MRK-740 is more selective for PRDM9 than other histone methyltransferases and other non-epigenetic targets. MRK-740 reduces PRDM9-dependent trimethylation of H3K4 (IC50?=?0.8?μM).
    MRK-740
  • HY-100565
    SGC2085
    		Inhibitor 99.46%
    SGC2085 is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins.
    SGC2085
  • HY-155170
    MTDH-SND1 blocker 1
    		Inhibitor 99.33%
    MTDH-SND1 blocker 1 (compound C26-A6) is an inhibitor of the MTDH-SND1 protein. MTDH-SND1 blocker 1 inhibits cancer metastasis.
    MTDH-SND1 blocker 1
  • HY-153191
    EZH2-IN-15
    		Inhibitor 99.18%
    EZH2-IN-15 is a EZH2 inhibitor. EZH2-IN-15 has anti-tumor activity, and can be used for research of H3K27me3-dependent tumors.
    EZH2-IN-15
  • HY-129441
    Metoprine
    		Inhibitor 99.67%
    Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine, a diaminopyrimidine derivative, can cross the blood-brain barrier and increase brain histamine levels by inhibiting HMT. Metoprine is an antifolate and antitumor agent.
    Metoprine
Cat. No. Nom du produit / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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