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-124699
    MMSET-IN-1
    		Inhibitor
    MMSET-IN-1 is a multiple myeloma SET domain (MMSET, aka NSD2/WHSC1) inhibitor against SETD2 and MMSET with IC50s of 0.49 and 3.3 μM, respectively. MMSET-IN-1 has a Kd of 1.6 μM for MMSET.
    MMSET-IN-1
  • HY-170674
    ND-L11B free base
    		Degrader
    ND-L11B is a potent degrader of nuclear receptor binding SET domain protein 2 (NSD2) and RE-IIBP, with the DC50 of 1.48 and 0.8 μM, the Dmax is closed to 80 %.
    ND-L11B free base
  • HY-112080A
    (R)-BAY-6035
    		Inhibitor
    (R)-BAY-6035 is a novel inhibitor that selectively targets the methylation of MAP3K2 by SMYD3, demonstrating nanomolar potency and specificity against kinases and other protein lysine methyltransferases.
    (R)-BAY-6035
  • HY-163588
    PRMT5-IN-39
    		Inhibitor
    PRMT5-IN-39 (compound 107) is an orally active PRMT5 inhibitor and can be used for study of cancer.
    PRMT5-IN-39
  • HY-108998
    Bisaramil hydrochloride
    Bisaramil hydrochloride is an antiarrhythmic compound with activity in inhibiting free radical generation. Bisaramil hydrochloride directly blocks sodium currents and exhibits enhanced sodium channel blocking ability. Bisaramil hydrochloride inhibits isoproterenol-induced slow calcium action potentials in cardiomyocytes. Bisaramil hydrochloride reduces heart rate and prolongs the PR, QRS, and QT intervals in the electrocardiogram, showing blocking effects on sodium and potassium channels. Bisaramil hydrochloride reduces cardiac conduction velocity, increases the threshold current for capture and atrial fibrillation, and prolongs the effective refractory period. Bisaramil hydrochloride reduces ventricular arrhythmias and eliminates mortality caused by ventricular fibrillation in ischemic rat hearts.
    Bisaramil hydrochloride
  • HY-121103
    Aclantate
    Aclantate is a nonsteroidal anti-inflammatory drug with anti-inflammatory and analgesic activity. Aclantate is mainly used to relieve various types of pain and reduce inflammatory responses. Aclantate can be used to suppress rheumatoid arthritis and other related diseases.
    Aclantate
  • HY-168143
    YD1342
    		Inhibitor
    YD1342 is a prodrug of YD1130, which exhibits potent inhibitory effects on cellular substrate methylation, breast cancer cell clonogenicity, and tumor growth in animal models, exceeding or matching known PRMT4-specific inhibitors..
    YD1342
  • HY-168842
    PRMT5-IN-47
    		Inhibitor
    PRMT5-IN-47 (compound 20) is a potent, selectively and orally active, MTA cooperative PRMT5 inhibitor with an IC50 value of 15 nM. PRMT5-IN-47 shows antiproliferative activity. PRMT5-IN-47 shows anticancer activity.
    PRMT5-IN-47
  • HY-155221
    UNC7145
    		Control
    UNC7145 is an inactive derivative of UNC6934 (HY-145103) that can be used as a negative control for the protein-protein inhibition activity of UNC6934.
    UNC7145
  • HY-162665
    WIZ degrader 1
    		Inducer
    WIZ degrader 1 (Compound 141) is a degrader for widely interspaced zinc finger motifs (WIZ) with an AC50 of 2 nM. WIZ degrader 1 induces the expression of fetal hemoglobin (HbF) with an EC50 of 6 mM. WIZ degrader 1 is used in research of inherited blood disorders.
    WIZ degrader 1
  • HY-P990434
    Anti-Histone H3 Antibody
    		Inhibitor
    The Anti-Histone H3 Antibody is a CHO-expressed humanized antibody that targets Histone H3. The Anti-Histone H3 Antibody has a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for the Anti-Histone H3 Antibody can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-Histone H3 Antibody
  • HY-144188
    PRMT5-IN-17
    		Inhibitor
    PRMT5-IN-17 (Compound 6) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification.
    PRMT5-IN-17
  • HY-161419
    EZH2-IN-18
    		Inhibitor
    EZH2-IN-18 (compound 9e) is a potent inhibitor of enhancer of zeste homologue 2 (EZH2WT) , with the IC50 of 1.01 nM. EZH2-IN-18 shows inhibition in proliferation and induction in apoptosis in tumor cells.
    EZH2-IN-18
  • HY-113786
    EZH2-IN-21
    		Inhibitor
    EZH2-IN-21 is a potent inhibitor of the histone lysine methyltransferase enhancer of zeste homologue 2 (EZH2) with anticancer activity. EZH2-IN-21 is competitive with the cofactor SAM and noncompetitive with peptide or nucleosome substrates.
    EZH2-IN-21
  • HY-149005
    PRMT5-IN-19
    		Inhibitor
    PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research.
    PRMT5-IN-19
  • HY-163561
    CARM1-IN-6
    		Inhibitor
    CARM1-IN-6 (iCARM1) is an effective and selective inhibitor of CARM1 with an IC50 value of 12.3 μM. CARM1-IN-6 exhibits cell growth inhibitory activity and can be used in cancer research.
    CARM1-IN-6
  • HY-116708
    DCE_254
    		Inhibitor
    DCE_254 is an EZH2 inhibitor (IC50=11 μM) that also exhibits significant antiproliferative activity against lymphoma cell lines. DCE_254 inhibits the development of hypermethylation-related cancers by inhibiting the SAM-mediated methyl transfer process (IC50=10.3 μM).
    DCE_254
  • HY-141566
    EZH2-IN-5
    		Inhibitor
    EZH2-IN-5 is a potent EZH2 inhibitor with IC50 values of 1.52 nM and 4.07 nM for wild-type and mutant Tyr641 EZH2, respectively.
    EZH2-IN-5
  • HY-144187
    PRMT5-IN-16
    		Inhibitor
    PRMT5-IN-16 (Compound 20) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification.
    PRMT5-IN-16
  • HY-150400
    XF056-132 free base
    		Inhibitor
    XF056-132 free base is a potent WDR5 (WD40 repeat domain protein 5) PROTAC degrader.
    XF056-132 free base
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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