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-12186G
    3-Deazaneplanocin A hydrochloride (GMP)
    		Inhibitor
    3-Deazaneplanocin A (DZNep) hydrochloride (GMP) is 3-Deazaneplanocin A hydrochloride (HY-12186) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 3-Deazaneplanocin A hydrochloride is a potent histone methyltransferase EZH2 inhibitor.
    3-Deazaneplanocin A hydrochloride (GMP)
  • HY-113846
    CMP-5 hydrochloride
    		Inhibitor
    CMP-5 hydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 hydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 hydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected.
    CMP-5 hydrochloride
  • HY-122181A
    OTS186935 trihydrochloride
    		Inhibitor
    OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells.
    OTS186935 trihydrochloride
  • HY-111810
    SMYD2-IN-1
    		Inhibitor
    SMYD2-IN-1 is a SMYD2 inhibitor extracted from patent WO2016166186A1, compound example 1.1, has an IC50 of 4.45 nM.
    SMYD2-IN-1
  • HY-108239
    BIX-01294 trihydrochloride
    		Inhibitor
    BIX-01294 trihydrochloride is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 trihydrochloride inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294 trihydrochloride, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 trihydrochloride has antitumor activity in recurrent tumor cells.
    BIX-01294 trihydrochloride
  • HY-153057
    PRMT5-IN-46
    		Inhibitor
    PRMT5-IN-46 (compound 278) inhibits PRMT5 with IC50 of 1-10 μM. PRMT5 is a methyltransferase which is associated with specific genetic alterations. PRMT5-IN-46 can be used to treat proliferative diseases, metabolic disorders, and blood diseases.
    PRMT5-IN-46
  • HY-156292
    IHMT-EZH2-426
    		Inhibitor
    IHMT-EZH2-426 (compound 38) is an effective covalent EZH2 degrader, with IC50 values of 1.3 nM, 1.2 nM, and 1.7-3.5 nM for EZH2 wild type, EZH2-A687V, and EZH2-Y641F/Y641N/Y641S, respectively. IHMT-EZH2-426 reduces H3K27me3 and EZH2 levels and shows effective anti-proliferative effects in B-cell lymphoma and TNBC cell lines.
    IHMT-EZH2-426
  • HY-103641B
    (2R)-Octyl-α-hydroxyglutarate sodium
    		Control
    (2R)-Octyl-α-hydroxyglutarate (sodium) is the sodium salt form of (2R)-Octyl-α-hydroxyglutarate. (2R)-Octyl-α-hydroxyglutarate has anti-inflammatory effects.
    (2R)-Octyl-α-hydroxyglutarate sodium
  • HY-146187
    Antitumor agent-69
    		Inhibitor
    Antitumor agent-69 (compound 12) is a potent inhibitor of protein-protein interaction between DOT1L and MLL-AF9/MLL-ENL, with Kis of 9 nM and 109 nM for AF9 and ENL, respectively. Antitumor agent-69 exhibits anticancer cellular activitiy.
    Antitumor agent-69
  • HY-163799
    PRMT5-MTA-IN-1
    		Inhibitor
    PRMT5-MTA-IN-1 (Compound A9a) is an inhibitor for protein arginine methyltransferase PRMT5-MTA. PRMT5-MTA-IN-1 inhibits the proliferation of colorectal cancer cell HCT116 wildtype and MTAP del mutant, with an IC50 of 16 nM and 2.47 μM. PRMT5-MTA-IN-1 exhibits good liver microsomal stability and film permeability. PRMT5-MTA-IN-1 exhibits good pharmacokinetic characteristics in CD-1 mice.
    PRMT5-MTA-IN-1
  • HY-155051
    Antiproliferative agent-25
    		Inhibitor
    Antiproliferative agent-25 (Compound 3s4) is a selective PRMT5 inhibitor (IC50: 0.11 μM). Antiproliferative agent-25 up-regulates hnRNP E1 protein level. Antiproliferative agent-25 forms H-bond interactions with SAM and E444 residue of PRMT5. Antiproliferative agent-25 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. Antiproliferative agent-25 has high clearances with T1/2 of only 21.8 and 4.7 min in human and rat liver microsomes.
    Antiproliferative agent-25
  • HY-121029
    Bisegliptin
    Bisegliptin (KRP-104) is a small molecule compound with antidiabetic activity. Bisegliptin is metabolized mainly by converting the cyano group to the carboxylic acid form, and DPP-4 plays a partial role in its metabolism. The carboxylic acid metabolite of bisegliptin can be detected both in vivo and in vitro. In rat experiments, the plasma concentration of the carboxylic acid metabolite of bisegliptin was affected by other DPP inhibitors, showing the complexity of its metabolic process. The amide intermediate of bisegliptin was detected both in vivo and in vitro, and its conversion rate was significantly faster than that of the parent compound when incubated with DPP-4.
    Bisegliptin
  • HY-114208
    BI-9321
    		Antagonist
    BI-9321 is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells.
    BI-9321
  • HY-169078
    ML234
    		Inhibitor
    ML234 is a dual inhibitor against EZH2/LSD1 with IC50 values of 0.09 and 0.12 μM, respectively. ML234 displays an excellent antiproliferative capacity against prostate cancer cell lines LNCAP, PC3 and 22RV1. ML234 suppresses the tumor growth in the 22RV1 xenograft mouse model. ML234 is promising for research of anticancer agents in prostate cancer.
    ML234
  • HY-163587
    PRMT5-IN-39-d3
    		Inhibitor
    PRMT5-IN-39-d3 is the deuterated form of PRMT5-IN-39. PRMT5-IN-39-d3 is an orally active PRMT5 inhibitor and can be used for study of cancer.
    PRMT5-IN-39-d<sub>3</sub>
  • HY-169958
    EZH2-IN-22
    		Inhibitor
    EZH2-IN-22 (example 92) is a potent EZH2 inhibitor with IC50 values of <0.00051, <0.00051, 0.00052 µM for EZH2 (Y641N), EZH2 (Y641F), EZH2 (wt), respectively. EZH2-IN-22 shows antiproliferation activity.
    EZH2-IN-22
  • HY-144189
    PRMT5-IN-18
    		Inhibitor
    PRMT5-IN-18 (Compound 002) is a potent PRMT5 inhibitor that can be used for the research of a disease mediated by PRMT5， such as cancer.
    PRMT5-IN-18
  • HY-157332
    WDR5-IN-7
    		Inhibitor
    WDR5-IN-7 (Compound 22) is an orally bioavailable benzoxazepinone-based WD repeat domain 5 (WDR5) inhibitor. WDR5-IN-7 can be used for the research of anti-cancer.
    WDR5-IN-7
  • HY-150680
    SARS-CoV-2 nsp14-IN-1
    		Antagonist
    SARS-CoV-2 nsp14-IN-1 (Compound 3) is a prototypic bisubstrate inhibitor of SARS-CoV-2 Nsp14 MTase with an IC50 value of 0.061 μM. SARS-CoV-2 nsp14-IN-1 (Compound 3) has an excellent selectivity profile over a panel of human methyltransferases, can against apanel of 10 human MTases including histone lysine, proteinarginine, and DNA and RNA MTases.
    SARS-CoV-2 nsp14-IN-1
  • HY-154854
    BBDDL2059
    		Inhibitor
    BBDDL2059 is a selective covalent inhibitor of histone methyltransferase EZH2 with an IC50 of 1.5 nM for EZH2-Y641F. BBDDL2059 inhibits lymphoma cell growth at nanomolar concentrations and can be used for anticancer research.
    BBDDL2059
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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