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-144858
    EZM0414
    		Inhibitor 99.11%
    EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 (IC50=18 nM in SETD2 biochemical assay; IC50=34 nM in cellular assay). EZM0414 can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma.
    EZM0414
  • HY-107777
    LLY-283
    		Inhibitor 98.93%
    LLY-283, a chemical probe, 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-111109
    EZM 2302
    		Inhibitor 99.51%
    EZM 2302 is a potent and orally active CARM1 inhibitor with an IC50 value of 6 nM. EZM 2302 shows antiproliferative activity and anti-tumor activity. EZM 2302 inhibits PABP1 and SMB expression.
    EZM 2302
  • 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-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, a chemical probe, 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-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-158102
    Rinzimetostat
    		Inhibitor 99.90%
    Rinzimetostat (ORIC-944) is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). Rinzimetostat is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer.
    Rinzimetostat
  • HY-147081
    AS 1411
    		Inhibitor 99.52%
    AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity.
    AS 1411
  • HY-10929
    UNC0224
    		Inhibitor 98.93%
    UNC0224 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 2.6 nM, an IC50 of 15 nM and a Kd of 23 nM. UNC0224 also potently inhibits b>GLP with assay-dependent IC50 values of 20-58 nM. UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E.
    UNC0224
  • HY-148669
    Bleximenib
    		Inhibitor 99.36%
    Bleximenib (JNJ-75276617) is an orally active and selective menin-KMT2A inhibitor, with IC50 values of 0.1 nM, 0.045 nM, and ≤0.066 nM for humans, mice, and dogs, respectively. Bleximenib can inhibit the proliferation and induce apoptosis and differentiation of tumor cells. Bleximenib can be used in the research of tumors such as leukemia.
    Bleximenib
  • 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-103663
    MAK683
    		Inhibitor 99.02%
    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-101496
    MT-DADMe-ImmA
    		Inhibitor 99.17%
    MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM.
    MT-DADMe-ImmA
  • HY-B1322
    Amodiaquine dihydrochloride dihydrate
    		Inhibitor 99.92%
    Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
    Amodiaquine dihydrochloride dihydrate
  • HY-148419
    Ralometostat
    		Inhibitor 99.90%
    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-131493
    PF-06939999
    		Inhibitor 99.84%
    PF-06939999 (PRMT5-IN-3) is a SAM-competitive, orally active PRMT5 inhibitor that inhibits the expression of SDMA protein (IC50 in A427 is 1.1 nM). PF-06939999 exhibits antitumor effect.
    PF-06939999
  • 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-147081A
    AS 1411 sodium
    		Inhibitor 99.52%
    AS 1411 (AGRO-100) sodium is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 sodium inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 sodium reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. S 1411 sodium works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. S 1411 sodium-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity
    AS 1411 sodium
  • HY-148669A
    Bleximenib oxalate
    		Inhibitor 98.97%
    Bleximenib (JNJ-75276617) oxalate is an orally active and selective menin-KMT2A inhibitor, with IC50 values of 0.1 nM, 0.045 nM, and ≤0.066 nM for humans, mice, and dogs, respectively. Bleximenib oxalate can inhibit the proliferation and induce apoptosis and differentiation of tumor cells. Bleximenib oxalate can be used in the research of tumors such as leukemia.
    Bleximenib oxalate
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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