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-111589
    EPZ-4777
    		Inhibitor
    EPZ-4777 is a selective DOT1L inhibitor which inhibits H3K79 methylation in cancer cells, blocks the expression of leukemogenic genes, and selectively kills cells that contain the translocation. EPZ-4777 can be used for cancer research.
    EPZ-4777
  • HY-178028
    PRMT5-IN-53
    		Inhibitor
    PRMT5-IN-53 is a gut-restricted and orally active PRMT5 inhibitor with pIC50s of ≥ 9.7 against hPRMT5 and mPRMT5. PRMT5-IN-53 binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. PRMT5-IN-53 effectively inhibits PRMT5 locally in the intestines of mice, significantly reducing the number and area of polyps, while avoiding systemic hematological toxicity (such as anemia, neutropenia). PRMT5-IN-53 can be used for the study of colorectal cancer especially for familial adenomatous polyposis (FAP).
    PRMT5-IN-53
  • HY-145813
    MU1656
    		Inhibitor
    MU1656 is a potent and selective inhibitor of histone methyltransferase DOT1L, with an IC50 of 2 nM. MU1656 can be used for the research of hematological malignancies.
    MU1656
  • HY-176135
    BBDDL2204
    		Inhibitor
    BBDDL2204 (compound 13) is a potent and selective EZH2 covalent inhibitor. BBDDL2204 inhibits EZH2Y641F with an IC50 of 2.5 nM.
    BBDDL2204
  • HY-100565A
    SGC2085 hydrochloride
    		Inhibitor
    SGC2085 hydrochloride is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 hydrochloride also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins.
    SGC2085 hydrochloride
  • HY-181914
    UNC7242
    		Antagonist
    UNC7242 is an antagonist that binds to the Tudor domains of PHF1 and PHF19, with a Kd of 1.13 μM for PHF1 and 0.64 μM for PHF19. UNC7242 fails to displace full-length PHF1 or PHF19 from H3K36me3 nucleosomes or chromatin. UNC7242 can be used in studies related to multiple myeloma, endometrial stromal sarcoma, and ossifying fibromyxoid tumor.
    UNC7242
  • HY-142094
    NSD3-IN-2
    		Inhibitor
    NSD3-IN-2 is a potent NSD3 inhibitor with an IC50 value of 17.97 μM. NSD3-IN-2 inhibits the growth and proliferation of non-small cell lung cancer cell lines H460, H1299 and H1650 with anti-cancer activity.
    NSD3-IN-2
  • HY-177497
    SKLB-03220
    		Inhibitor
    SKLB-03220 is a selective and orally active EZH2 covalent inhibitor with an IC50 of 1.72 nM for EZH2MUT. SKLB-03220 exhibits weak activities against other tested histone methyltransferases (HMTs) and kinases. SKLB-03220 displays noteworthy potency against ovarian cancer cell lines and induces cell apoptosis. SKLB-03220 significantly inhibits tumor growth in PA-1 xenograft model. SKLB-03220 can be used for the study of ovarian cancer.
    SKLB-03220
  • HY-13689G
    Go 6983 (GMP)
    		Inhibitor
    Go 6983 GMP is Go 6983 (HY-13689) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Go 6983 is a dual inhibitor targeting Suv39h1/2 (KMT1A/KMT1B) and PKC, as well as a transcriptional activator capable of inducing DNA hypomethylation. Go 6983 stimulates the transcription of Prdm14 by reducing Suv39h1/2 protein levels, decreasing histone modifications in the Prdm14 promoter region, and increasing the recruitment of RNA polymerase II. Go 6983 induces genome-wide DNA hypomethylation by inhibiting de novo methyltransferase expression and increasing Tet1/Tet2 levels, thereby promoting self-renewal and pluripotency maintenance of stem cells. Meanwhile, Go 6983 can block PKC-mediated signaling pathways to reduce the expression of EMT-related genes and eliminate the upregulation of antioxidant genes downstream of NRF2. Go 6983 is mainly used in mechanism studies related to myocardial ischemia/reperfusion injury.
    Go 6983 (GMP)
  • HY-172614
    RK-0080552
    		Inhibitor
    RK-0080552 (RK-552) is a NSD2 inhibitor with an IC50 of 0.11 μM, and it exhibits selectivity over histone methyltransferases G9a (IC50: 1.2 μM) and SET7/9 (IC50: >50 μM). RK-0080552 functionally inhibits NSD2 histone methyltransferase activity, reduces the dimethylation level of histone H3 lysine 36, suppresses IRF4 transcription, induces apoptosis and triggers cell death. RK-0080552 inhibits the growth of xenograft tumors and prolongs host survival. RK-0080552 is available for the research of multiple myeloma.
    RK-0080552
  • HY-183951
    TNG456
    		Inhibitor
    TNG456 is an orally active, CNS-penetrant, selective, MTA-cooperative PRMT5 inhibitor. TNG456 drives dose-dependent antitumor activity in mouse xenograft models. TNG456 can be used for the research of MTAP-null solid tumors, including gliomas, and CNS metastases.
    TNG456
  • HY-181357
    PROTAC EZH2 Degrader-29
    		Degrader
    PROTAC EZH2 Degrader-29 (compound 66) is a is a PROTAC protein degrader targeting EZH2 with an IC50 of 24.53 μM against diffuse large B-cell lymphoma cells. PROTAC EZH2 Degrader-29 can be used in studies related to diffuse large B-cell lymphoma.
    PROTAC EZH2 Degrader-29
  • HY-175871
    (Rac)-NSD2-PWWP1-IN-4
    		Inhibitor
    (Rac)-NSD2-PWWP1-IN-4 (compound 7) is an effective NSD2-PWWP1 inhibitor IC50 and Kd values are 0.21 and 0.15 μM. (Rac)-NSD2-PWWP1-IN-4 can be used in tumor research.
    (Rac)-NSD2-PWWP1-IN-4
  • HY-145452
    5-Octyl-α-ketoglutarate
    5-Octyl-α-ketoglutarate (5-Octyl 2-oxopentanedioate) is a cell-permeable substrate for lysine demethylase. 5-Octyl-α-ketoglutarate is related to protein demethylation, inhibits cell proliferation of wtCRBN expressing cells, and also enhances Lenalidomide (HY-A0003)-induced sensitivity and inhibits myeloma (MM) ) drug resistance of cells. When myeloma (MM) cells undergo glutamine-dependent proliferation, α-ketoglutarate increases glutamine catabolism to promote protein demethylation.
    5-Octyl-α-ketoglutarate
  • HY-176231
    PRMT5-IN-51
    		Inhibitor
    PRMT5-IN-51 (compound 16–19F) is a potent PRMT5 inhibitor. PRMT5-IN-51 shows antiproliferative activity.
    PRMT5-IN-51
  • HY-158157
    ZL-28-6
    		Inhibitor
    ZL-28-6 is a type I PRMT inhibitor (IC50: 18 nM). ZL-28-6 effectively targets CARM1 (a member of PRMT) within cells and can be used for cancer research.
    ZL-28-6
  • HY-173092
    PRMT5 ligand 1
    		Ligand
    PRMT5 ligand 1 (compound 3) is the ligand for PRMT5 that can be used as target protein ligand for synthesis of PROTAC degrader MS4322 (HY-141877).
    PRMT5 ligand 1
  • HY-N2420R
    Flavokawain A (Standard)
    		Inhibitor
    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 (Standard)
  • HY-107574R
    TC-E 5003 (Standard)
    		Inhibitor
    TC-E 5003 (Standard) is the analytical standard of TC-E 5003 (HY-107574). This product is intended for research and analytical applications. TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 1.5 µM against hPRMT1. TC-E 5003 modulates the lipopolysaccharide (LPS) (HY-D1056)-induced AP-1 and NF-κB signaling pathways with anti-inflammatory properties. TC-E 5003 also upregulates the expression of Ucp1 and Fgf21, activates protein Kinase A signaling and lipolysis in primary subcutaneous adipocytes from both mouse and humans. TC-E 5003 is promising for research of obesity and associated metabolic disorders, oxidative stress, inflammation and cancers.
    TC-E 5003 (Standard)
  • HY-118715
    Setin-1
    		Inhibitor
    Setin-1 is one of the most potent inhibitors of Set7, acting by inhibiting KMTase G9a.
    Setin-1
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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