2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase

Histone Methyltransferase

Histone Methyltransferase

Related Products

PDF 2.85 MB

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-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-139626
    EPZ-719
    		Inhibitor 99.00%
    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-147525
    PROTAC EZH2 Degrader-1
    		Inhibitor 99.44%
    PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes.
    PROTAC EZH2 Degrader-1
  • HY-107574
    TC-E 5003
    		Inhibitor 98.03%
    TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 1.5 µM against hPRMT1. TC-E 5003 modulates the lipopolysaccharide (LPS) (HY-D1056)-induced AP-1 and NF-κB signaling pathways with anti-inflammatory properties. TC-E 5003 also upregulates the expression of Ucp1 and Fgf21, activates protein kinase A signaling and lipolysis in primary subcutaneous adipocytes from both mouse and humans. TC-E 5003 is promising for research of obesity and associated metabolic disorders, oxidative stress, inflammation and cancers.
    TC-E 5003
  • HY-110137
    Furamidine dihydrochloride
    		Inhibitor ≥99.0%
    Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent.
    Furamidine dihydrochloride
  • HY-W011927
    4,4'-Sulfonyldiphenol
    		Agonist 99.81%
    4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone), a substitute for Bisphenol A (HY-18260), is widely used in industrial and consumer products. 4,4'-Sulfonyldiphenol is an oally ative estrogen receptor (ER) agonist and can competitively bind to thyroid hormone receptors (TR) with IC50 values for TRα and TRβ are 2650 μM and 2294 μM respectively, thereby affecting breast development and reducing the expression of androgen receptor (AR) in fetal testes. 4,4'-Sulfonyldiphenol promotes the progression of glioblastoma by upregulating the EZH2 mediated PI3K/AKT/mTOR pathway. Under chronic exposure, 4,4'-Sulfonyldiphenol can cause significant lipid deposition and dyslipidemia in the mouse liver by upregulating JunB and Atf3, and has a role in causing obesity at low doses. 4,4'-Sulfonyldiphenol induces intestinal inflammation by altering the intestinal microbiome. 4,4'-Sulfonyldiphenol accelerates the progression of atherosclerosis in zebrafish embryo larvae.
    4,4'-Sulfonyldiphenol
  • HY-19313
    LLY-507
    		Inhibitor 98.47%
    LLY-507 is a potent and selective inhibitor of protein-lysine methyltransferase SMYD2. LLY-507 potently inhibits the ability of SMYD2 to methylate p53 peptide with an IC50 <15 nM. LLY-507 serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes.
    LLY-507
  • HY-21972
    BCI-121
    		Inhibitor 99.89%
    BCI-121 is a SMYD3 inhibitor that impairs the proliferation of cancer cell.
    BCI-121
  • 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-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-13808
    UNC 0631
    		Inhibitor 99.27%
    UNC 0631 is a potent histone methyltransferase G9a inhibitor with an IC50 of 4 nM. UNC 0631 potently reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 25 nM.
    UNC 0631
  • HY-B1322B
    Amodiaquine dihydrochloride
    		Inhibitor 99.97%
    Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a Ki of 18.6 nM. Amodiaquine dihydrochloride 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
  • HY-139400
    Pociredir
    		Inhibitor 99.97%
    Pociredir (FTX-6058) is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). Pociredir can induce HbF protein expression in cell and murine models. Pociredir can be used for the research of select hemoglobinopathies, including sickle cell disease and β-thalassemia.
    Pociredir
  • HY-148669A
    Bleximenib oxalate
    		Inhibitor 98.0%
    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
  • 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-15226
    AZ505
    		Inhibitor 99.99%
    AZ505 is a potent and selective SMYD2 inhibitor with an IC50 of 0.12 μM.
    AZ505
  • HY-12970A
    EPZ020411 hydrochloride
    		Inhibitor 98.15%
    EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer.
    EPZ020411 hydrochloride
  • HY-162275
    JMJD1C-IN-1
    		Activator 99.99%
    JMJD1C-IN-1 is an orally active and selective inhibitor of JMJD1C (IC50 = 0.59 μM, Kd = 1.96 μM). JMJD1C-IN-1 inhibits the binding of JMJD1C to H3K9me2 peptide substrate in the HTRF assay (IC50 = 1.47 μM). JMJD1C-IN-1 disrupts intratumoral regulatory T (Treg) cell fitness by dual mechanisms: promoting H3K9me2 accumulation to downregulate PD1 expression and reducing STAT3 demethylation to enhance STAT3 activation. JMJD1C-IN-1 demonstrates dose-dependent antitumor efficacy in multiple mouse tumor models (MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatocellular carcinoma, CT26 colorectal cancer). JMJD1C-IN-1 can be used for the study of tumor immunotherapy by selectively targeting intratumoral Treg cells.
    JMJD1C-IN-1
  • 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-145602
    Tulmimetostat
    		Inhibitor 99.79%
    Tulmimetostat (CPI-0209) is an orally active EZH1/EZH2 inhibitor that targets and inhibits the EZH2 enzyme.Tulmimetostat has antitumor activity and is used in a variety of solid tumor studies.
    Tulmimetostat
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.