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-112445
    SGC3027
    		Inhibitor 98.06%
    SGC3027 is a histone methyltransferase inhibitor. SGC3027 is the first potent, selective and cell active chemical probe for PRMT7.
    SGC3027
  • HY-101496
    MT-DADMe-ImmA
    		Inhibitor 98.42%
    MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM.
    MT-DADMe-ImmA
  • HY-101925
    CM-272
    		Inhibitor 98.70%
    CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death.
    CM-272
  • HY-107777
    LLY-283
    		Inhibitor 99.22%
    LLY-283 is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity.
    LLY-283
  • HY-100034
    NSC 663284
    		Inhibitor 99.29%
    NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively. NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM).
    NSC 663284
  • HY-12970
    EPZ020411
    		Inhibitor 98.07%
    EPZ020411 is a selective inhibitor of PRMT6 with an IC50 of 10 nM, has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 can be used for the research of cancer.
    EPZ020411
  • HY-101512
    A-395
    		Inhibitor 99.12%
    A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM.
    A-395
  • HY-148419
    Ralometostat
    		Inhibitor 98.89%
    TNG908 is a MTAP synergistic PRMT5 inhibitor. TNG908 crosses the blood-brain barrier and is orally active. TNG908 could be used in cancer research.
    Ralometostat
  • HY-18627A
    PFI-2 hydrochloride
    		Inhibitor 99.48%
    PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0  nM and (S)-PFI-2 shows inhibiting activity with IC50  value of 1.0  μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis.
    PFI-2 hydrochloride
  • HY-150190
    F5446
    		Inhibitor 99.38%
    F5446 (Compound 1) is a selective small molecule inhibitor of SUV39H1 methyltransferase. F5446 decreases H3K9me3 deposition at the FAS promoter, increases Fas expression and increases colorectal carcinoma cell sensitivity to FasL-induced apoptosis in vitro. F5446 suppresses human colon tumor xenograft growth in vivo.
    F5446
  • HY-B1322A
    Amodiaquine
    		Inhibitor 99.98%
    Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
    Amodiaquine
  • HY-18962
    AMI-1
    		Inhibitor ≥98.0%
    AMI-1 is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
    AMI-1
  • HY-109108A
    Valemetostat tosylate
    		Inhibitor 99.84%
    Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma.
    Valemetostat tosylate
  • HY-141429A
    AS-99 TFA
    		Inhibitor 99.15%
    AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.
    AS-99 TFA
  • HY-130708
    UNC6852
    		Inhibitor 99.60%
    UNC6852 is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a von Hippel-Lindau ligand, with an IC50 of 247 nM for EED.
    UNC6852
  • HY-103663
    MAK683
    		Inhibitor 99.18%
    MAK683 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
  • HY-116522
    AR420626
    		98.29%
    AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3) (IC50=117 nM). AR420626 has anti-inflammatory, anticancer and antidiabetic activities. AR420626 improves neurogenic diarrhea by inhibiting nAChR mediated neural pathways. AR420626 inhibits the growth of HepG2 xenografts and inhibits the proliferation of hepatoma cells by inducing apoptosis. AR420626 also suppresses allergic asthma and eczema and has the ability to activate GPR41 to increase Ca2+ signal-mediated glucose uptake and improve diabetes.
    AR420626
  • HY-139626
    EPZ-719
    		Inhibitor 99.85%
    EPZ-719 is a selective, orally effective SETD2 inhibitor with an IC50 value of 0.005 μM. EPZ-719 has anticancer activity.
    EPZ-719
  • HY-15226
    AZ505
    		Inhibitor 99.99%
    AZ505 is a potent and selective SMYD2 inhibitor with an IC50 of 0.12 μM.
    AZ505
  • HY-122181B
    OTS186935 hydrochloride
    		Inhibitor 99.22%
    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
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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