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-12845
    UNC2400
    		Inhibitor 99.92%
    UNC2400 is a close analog of UNC1999 with >1,000-fold lower potency than UNC1999 as a negative control for cell-based studies.
    UNC2400
  • HY-148674
    AM-9747
    		Inhibitor 99.76%
    AM-9747 (compound 503) is a potent PRMT5 inhibitor with an Ki value of 0.06 nM. AM-9747 shows antiproliferative.
    AM-9747
  • HY-155170
    MTDH-SND1 blocker 1
    		Inhibitor 99.33%
    MTDH-SND1 blocker 1 (compound C26-A6) is an inhibitor of the MTDH-SND1 protein. MTDH-SND1 blocker 1 inhibits cancer metastasis.
    MTDH-SND1 blocker 1
  • HY-12856
    GSK503
    		Inhibitor 99.52%
    GSK503 is a potent and specific inhibitor of EZH2 methyltransferase with Kiapp values of 3 to 27 nM.
    GSK503
  • HY-15227A
    EPZ004777 hydrochloride
    		Inhibitor 99.46%
    EPZ004777 hydrochloride is a potent, selective DOT1L inhibitor with an IC50 of 0.4 nM.
    EPZ004777 hydrochloride
  • HY-130615
    PROTAC EED degrader-2
    		Inhibitor 99.90%
    PROTAC EED degrader-2 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.11) targeting the EED subunit.
    PROTAC EED degrader-2
  • HY-N2420
    Flavokawain A
    		Inhibitor 99.93%
    Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.
    Flavokawain A
  • HY-122096
    DCLX069
    		Inhibitor 98.03%
    DCLX069 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 value of 17.9 µM. DCLX069 shows less active against PRMT4 and PRMT6. DCLX069 has anticancer effects.
    DCLX069
  • HY-114340
    LEM-14
    		Inhibitor 98.02%
    LEM-14 is a potent and selective NSD2 inhibitor with an IC50 of 132 µM. LEM-14 has very weak activitv against NSD1 and has no activity against NSD3. LEM-14 inhibits fibrotic gene expression in ND but not DIO BMDMs. LEM-14 combined with ionizing radiation (IR) enhances the apoptosis rate and reduces the colony-formation ability of CRC cells. LEM-14 exhibits enhanced anti-tumor efficacy in Balb/c nude mice bearing LoVo cell xenografts when combined with ionizing radiation. LEM-14 has the potential for the research of multiple myeloma and colorectal cancer.
    LEM-14
  • HY-100360
    MS049
    		Inhibitor 98.0%
    MS049, a chemical probe, is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells.
    MS049
  • HY-124131
    DS-437
    		Inhibitor 99.22%
    DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3.
    DS-437
  • HY-125292
    NV03
    		Antagonist 99.77%
    NV03 is a potent and selective antagonist of Ubiquitin-like with PHD and RING finger domains 1 (UHRF1)-H3K9me3 interaction by binding to UHRF1 tandem tudor domain, with a Kd of 2.4 μM. NV03 is also a ligand for E3 ligase. NV03 can be studied in anticancer research.
    NV03
  • HY-15573
    EI1
    		Inhibitor 99.78%
    EI1 (KB-145943) is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
    EI1
  • HY-13807
    UNC0646
    		Inhibitor 99.38%
    UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC50 of 6 nM. UNC0646 is also a potent GLP inhibitor (IC50 <15 nM) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 26 nM.
    UNC0646
  • HY-155814
    EML734
    		Inhibitor 99.48%
    EML734 is a potent and selective PRMT7/9 inhibitor with IC50 values of 315 nM and 0.89 μM, respectively.
    EML734
  • HY-141430
    AS-85
    		Inhibitor 98.05%
    AS-85 is a potent ASH1L histone methyltransferase inhibitor (IC50=0.6 μM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SET domain, with the Kd value of 0.78 μM.
    AS-85
  • HY-117421A
    CM-579 trihydrochloride
    		Inhibitor
    CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells.
    CM-579 trihydrochloride
  • HY-147090
    Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH
    		Degrader 99.06%
    Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH (Compound 21b) incorporates a ligand for EZH2, and a PROTAC linker, which recruit E3 ligases. Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH (Compound 21b) can be used for the research of lymphoma.
    Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH
  • HY-122182
    OTS193320
    		Inhibitor 98.64%
    OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggers apoptotic cell death. Combination of OTS193320 with Doxorubicin (HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX.
    OTS193320
  • HY-100025A
    HLCL-61 hydrochloride
    		Inhibitor 99.87%
    HLCL-61 hydrochloride is a first-in-class inhibitor of protein arginine methyltransferase 5 (PRMT5).
    HLCL-61 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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