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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. Nombre del producto Efecto Pureza Chemical Structure
  • HY-152236
    PRMT6-IN-3
    		Inhibitor 99.66%
    PRMT6-IN-3 (compound 25) is a selective PRMT6 inhibitor with an IC50 value of 192 nM. PRMT6-IN-3 can induce apoptosis in cancer cells and has anticancer activity.
    PRMT6-IN-3
  • HY-144330
    TDI-6118
    		Inhibitor 99.08%
    TDI-6118 (Compound 5) is a potent brain-penetrant inhibitor of EZH2. EZH2-IN-12 has the potential for the research of central nervous system malignancies.
    TDI-6118
  • HY-A0298
    EZH2-IN-2
    		Inhibitor 98.51%
    EZH2-IN-2 (Example 69) is a EZH2 inhibitor with an IC50 and a TR-FRET IC50 of 64 nM and 20 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity.
    EZH2-IN-2
  • HY-153390A
    (R)-AMG-193
    		Inhibitor 98.53%
    (R)-AMG-193 is an isomer of AMG 193 (HY-153390). AMG 193 is an orally active MTA-cooperative PRMT5 inhibitor with antitumor activity. AMG 193, when complexed with MTA, preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting PRMT5 (IC50=0.107 μM), thereby protecting normal cells with wild-type MTAP.
    (R)-AMG-193
  • HY-120137
    CMP-5
    		Inhibitor 99.61%
    CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected.
    CMP-5
  • HY-101508
    GNA002
    		Inhibitor 98.02%
    GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes.
    GNA002
  • HY-121093
    DC-S239
    		Inhibitor 99.73%
    DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC50 value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity.
    DC-S239
  • HY-112165
    PRMT5-IN-2
    		Inhibitor 98.68%
    PRMT5-IN-2 is a rotein arginine methyltransferase 5 (PRMT5) inhibitor extracted from patent WO2018130840A1, compound 3.
    PRMT5-IN-2
  • HY-176165
    CDK9/EZH2-IN-1
    		Inhibitor 99.08%
    CDK9/EZH2-IN-1 (Compound D16) is a CDK9/EZH2 dual-target inhibitor (IC50: 83.9/108.6 nM). CDK9/EZH2-IN-1 induces apoptosis and DNA double-strand breaks (DSBs). CDK9/EZH2-IN-1 inhibits the proliferation activity of MKN45, MDA-MB-453 and SW620 cancer cells (IC50 values are 136.3, 171.3 and 315.7 nM, respectively).
    CDK9/EZH2-IN-1
  • HY-131246
    DM-01
    		Inhibitor 98.05%
    DM-01 is a powerful and selective EZH2 inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors.
    DM-01
  • HY-119198
    NSC745885
    		Inhibitor 98.0%
    NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers.
    NSC745885
  • HY-101520A
    Dot1L-IN-1 TFA
    		Inhibitor 99.59%
    Dot1L-IN-1 TFA is a highly potent and selective Dot1L inhibitor with a Ki of 2 pM and an IC50 of <0.1 nM. Dot1L-IN-1 TFA potently suppresses H3K79 dimethylation (IC50=3 nM), as well as the activity of the HoxA9 promoter (IC50=17 nM) in HeLa and Molm-13 cells, respectively.
    Dot1L-IN-1 TFA
  • HY-146999
    YM458
    		Inhibitor 99.16%
    YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer.
    YM458
  • HY-15647
    BRD9539
    		Inhibitor 99.73%
    BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1.
    BRD9539
  • HY-156285
    ZZM-1220
    		Inhibitor 98.74%
    ZZM-1220 is a histone lysine methyltransferase G9a/GLP covalent inhibitor with IC50s of of 458 nM and 924 nM, respectively. ZZM-1220 inhibits H3K9me2 in cells and significantly induces apoptosis of triple-negative breast cancer (TNBC) cells and blocks the cell cycle in the G2/M phase.
    ZZM-1220
  • HY-138886
    RL5a
    		Inhibitor 99.6%
    RL5a (compund C23) is a SETD8 inhibitor.
    RL5a
  • HY-111418
    EBI-2511
    		Inhibitor 98.67%
    EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC50 of 6 nM in Pfeffiera cell lines, respectively.
    EBI-2511
  • HY-128579
    DW14800
    		Inhibitor 99.12%
    DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity.
    DW14800
  • HY-100757
    CPUY074020
    		Inhibitor 98.56%
    CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity.
    CPUY074020
  • HY-132233A
    DDO-2093 dihydrochloride
    		Inhibitor 98.79%
    DDO-2093 dihydrochloride is a potent MLL1-WDR5 protein-protein interaction inhibitor (IC50=8.6 nM; Kd=11.6 nM) with antitumor activity. DDO-2093 dihydrochloride selectively inhibits the catalytic activity of MLL complex.
    DDO-2093 dihydrochloride
Cat. No. Nombre del producto / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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