2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase
  5. Histone Methyltransferase Isoform
  6. Histone Methyltransferase Inhibitor

Histone Methyltransferase Inhibitor

Histone Methyltransferase Inhibitors (197):

Cat. No. Product Name Effect Purity
  • HY-113846A
    CMP-5 dihydrochloride
    		Inhibitor
    CMP-5 dihydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 dihydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 dihydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected.
  • HY-165496
    KAT-IN-2
    		Inhibitor
    KAT-IN-2 (7) is a potent and selective kynurenine aminotransferase II (KATII) inhibitor.
  • HY-12707B
    Piribedil maleate
    		Inhibitor
    Piribedil maleate is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil maleate is also a α2-adrenoceptors antagonist. Piribedil maleate can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil maleate has the potential for the research of parkinson's disease, circulatory disorders, cancers.
  • HY-111085
    CPI-905
    		Inhibitor
    CPI-905 is a potent, selective, and cell-active EZH2 inhibitor.
  • HY-100235A
    GSK591 hydrochloride
    		Inhibitor
    GSK591 (EPZ015866) hydrochloride is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 4 nM.
  • HY-12707R
    Piribedil (Standard)
    		Inhibitor
    Piribedil (Standard) is the analytical standard of Piribedil. This product is intended for research and analytical applications. Piribedil is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil is also a α2-adrenoceptors antagonist. Piribedil can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil has the potential for the research of parkinson's disease, circulatory disorders, cancers.
  • HY-110093
    UNC0638 hydrate
    		Inhibitor
    UNC0638 hydrate selectively inhibits G9a and GLP histone methyltransferases with IC50 of 15 nM and 19 nM, respectively. UNC0638 hydrate inhibits TNBC cell invasion and migration in vitro. UNC0638 hydrate is also an inhibitor of EHMT1/2 and induces fetal hemoglobin (HbF) expression in human erythroid progenitor cell culture. In addition, UNC0638 hydrate has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities, with excellent potency and selectivity against multiple epigenetic and non-epigenetic targets.
  • HY-172369
    CARM1/IKZF3 ligand 1
    		Inhibitor
    CARM1/IKZF3 ligand 1 is the inhibitor for CARM1 that can be used as the target protein ligand for synthesis of PROTAC CARM1/IKZF3 degrader-1 (HY-172368).
  • HY-P10463
    ssK36
    		Inhibitor
    ssK36 is a supersubstrate peptide of the histone methyltransferase (SET) domain protein 2 (SETD2), and ssK36 is designed for the SETD2 protein, a specific PKMT. It is responsible in human cells for adding methyl groups to the 36th lysine residue of histone H3 (H3K36) to form H3K36me3. ssK36 can be methylated by SETD2 at a rate more than 100 times faster than the natural substrate H3K36. ssK36 can be used to study the catalytic mechanism of PKMTs, especially substrate specificity and catalytic efficiency.
  • HY-111030
    PRMT1-IN-2
    		Inhibitor
    PRMT1-IN-2 (RM65) is a potent PRMT1 inhibitor with an IC50 of 55.4 μM. PRMT1-IN-2 shows histone hypomethylation in HepG2 cells.
  • HY-W013500
    (1-Nitroethene-1,2-diyl)dibenzene
    		Inhibitor
    (1-Nitroethene-1,2-diyl)dibenzene (alpha-Nitrostilbene; α-Nitrostilbene) is an inhibitor of protein arginine methyltransferase 1 (PRMT1; IC50=11 μM in histone H4 methylation assay). It also inhibits histone H4 methylation by PRMT8, but not histone H3.1 methylation by CARM1 or Set7/9, at concentrations of 10 and 100 μM.
  • HY-122223
    EPZ030456
    		Inhibitor
    EPZ030456 is a potent and selective SMYD3 inhibitor with an IC50 of 48 nM. EPZ030456 can be used for cancer research.
  • HY-164500
    MC3629
    		Inhibitor
    MC3629 is an inhibitor of histone methyltransferase (EZH2) with anti-tumor activity. MC3629 inhibits SHH MB cancer cell proliferation and self-renewal and induces apoptosis. MC3629 can be used to study drug resistance in tumor aggressiveness.
  • HY-19546A
    (R)-BAY-598
    		Inhibitor
    (R)-BAY-598 ((R)-4) is a potent inhibitor of protein-lysine methyltransferase SMYD2, with the IC50 of 1.7 μM.
  • HY-169113
    EPZ032597
    		Inhibitor
    EPZ032597 is a selective and noncompetitive SMYD2 inhibitor with an IC50 value of 16 nM. EPZ032597 is promising for research of pancreatic ductal adenocarcinoma.
  • HY-P10425
    T2857W
    		Inhibitor
    T2857W is a mutant peptide that has inhibitory effect on KIX-MLL interaction (IC50=5.67 μM). T2857W can be used for protein-protein interaction (PPI) and for the study of diseases related to KIX-MLL interaction, such as leukemia, cancer, etc.
  • HY-121493
    TM2-115
    		Inhibitor 98.37%
    TM2-115 inhibits malaria parasite histone methyltransferases, resulting in rapid and irreversible parasite death.