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-121103
    Aclantate
    Aclantate is a nonsteroidal anti-inflammatory drug with anti-inflammatory and analgesic activity. Aclantate is mainly used to relieve various types of pain and reduce inflammatory responses. Aclantate can be used to suppress rheumatoid arthritis and other related diseases.
    Aclantate
  • HY-170831
    DS79932728
    		Inhibitor
    DS79932728 is an orally active inhibitor for G9a and GLP with IC50 of 12.6 nM and 75.7 nM. DS79932728 induces the production of γ-globin, thereby increasing the level of fetal hemoglobin (HbF). DS79932728 increases F-reticulocytes (F-rets) proportion and exhibits good oral absorption characteristics in cynomolgus monkey models.
    DS79932728
  • HY-168143
    YD1342
    		Inhibitor
    YD1342 is a prodrug of YD1130, which exhibits potent inhibitory effects on cellular substrate methylation, breast cancer cell clonogenicity, and tumor growth in animal models, exceeding or matching known PRMT4-specific inhibitors..
    YD1342
  • HY-117947
    (R)-OR-S1
    		Control
    (R)-OR-S1 is an isomer of OR-S1. The dual ZH1/2 inhibitors OR-S1 and OR-S2 exhibit strong inhibitory activity against both EZH1 and EZH2. OR-S1 and OR-S2 are highly selective methyltransferase inhibitors against EZH1 and EZH2, and they have very similar molecular features. Therefore, we investigated the effect of OR-S1 on acute myeloid leukemia (AML). We found that OR-S1 was able to induce cell differentiation and apoptosis in AML cells. These findings encouraged us to investigate whether functional LT-HSCs could survive PRC2-targeted therapy with OR-S1 or OR-S1 combined with cytarabine. The results showed that OR-S1 did not cause significant myelosuppression, and BM cells treated with the combination therapy were able to undergo normal hematopoiesis even 4 months after treatment. Therefore, temporary inhibition of EZH1 and EZH2 is clinically tolerable, making this combination therapy suitable for AML patients. AML is generally believed to originate from myeloid progenitor cells that inherit a large number of biological properties.
    (R)-OR-S1
  • HY-168842
    PRMT5-IN-47
    		Inhibitor
    PRMT5-IN-47 (compound 20) is a potent, selectively and orally active, MTA cooperative PRMT5 inhibitor with an IC50 value of 15 nM. PRMT5-IN-47 shows antiproliferative activity. PRMT5-IN-47 shows anticancer activity.
    PRMT5-IN-47
  • HY-155221
    UNC7145
    		Control
    UNC7145 is an inactive derivative of UNC6934 (HY-145103) that can be used as a negative control for the protein-protein inhibition activity of UNC6934.
    UNC7145
  • HY-181331
    PROTAC EZH2 Degrader-27
    		Inhibitor
    PROTAC EZH2 Degrader-27 is a EZH2 PROTAC inhibitor with an IC50 of 4.00 nM against EZH2. PROTAC EZH2 Degrader-27 inhibits methyltransferase activity by interacting with the SET domain of EZH2.
    PROTAC EZH2 Degrader-27
  • HY-162665
    WIZ degrader 1
    		Inducer
    WIZ degrader 1 (Compound 141) is a degrader for widely interspaced zinc finger motifs (WIZ) with an AC50 of 2 nM. WIZ degrader 1 induces the expression of fetal hemoglobin (HbF) with an EC50 of 6 mM. WIZ degrader 1 is used in research of inherited blood disorders.
    WIZ degrader 1
  • HY-P990434
    Anti-Histone H3 Antibody
    		Inhibitor
    The Anti-Histone H3 Antibody is a CHO-expressed humanized antibody that targets Histone H3. The Anti-Histone H3 Antibody has a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for the Anti-Histone H3 Antibody can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-Histone H3 Antibody
  • HY-119164
    DC-S238
    		Inhibitor
    DC-S238 is an orally active and highly selective histone methyltransferase SET7 (SETD7) inhibitor (IC50=4.88 μM). DC-S238 is promising for research of cancer, diabetes and inflammatory diseases.
    DC-S238
  • HY-144188
    PRMT5-IN-17
    		Inhibitor
    PRMT5-IN-17 (Compound 6) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification.
    PRMT5-IN-17
  • HY-161419
    EZH2-IN-18
    		Inhibitor
    EZH2-IN-18 (compound 9e) is a potent inhibitor of enhancer of zeste homologue 2 (EZH2WT) , with the IC50 of 1.01 nM. EZH2-IN-18 shows inhibition in proliferation and induction in apoptosis in tumor cells.
    EZH2-IN-18
  • HY-179446
    HP1-IN-2
    		Inhibitor
    HP1-IN-2 (Compound (R)-18) is a HP1/H3K9me3 interaction inhibitor with an IC50 of 18.1 μM. HP1-IN-2 can be used for studying various cancers with overexpression of HP1.
    HP1-IN-2
  • HY-181308
    PROTAC EZH2 Degrader-13
    		Degrader
    PROTAC EZH2 Degrader-13 is an EZH2-targeting PROTAC with an IC50 of 2.70 nM. PROTAC EZH2 Degrader-13 exerts antiproliferative effects in cancer cells. PROTAC EZH2 Degrader-13 can be used for the research of cancer.
    PROTAC EZH2 Degrader-13
  • HY-160423
    MS8815N
    		Control
    MS8815N is a negative control of EZH2 PROTAC degrader MS8815 (HY-148334). MS8815N is incapable of recruiting the VHL E3 ligase but retains the same EZH2 binding moiety and linker. MS8815N can be used for triple-negative breast cancer (TNBC) research.
    MS8815N
  • HY-186045
    SKLB06489
    		Inhibitor
    SKLB06489 is a selective and orally active inhibitor of type I PRMT enzymes, with IC50 values of 64.55 nM (PRMT1), 4.21 nM (PRMT6), and 51.27 nM (PRMT8). SKLB06489 inhibits cell proliferation, colony formation, DNA replication, and DNA damage repair in cancer cells. SKLB06489 induces G0/G1-phase cell cycle arrest and apoptosis in cancer cells. SKLB06489 enhances intracellular cholesterol efflux via ABCA1 and ABCG1 upregulation, disrupts cholesterol metabolic homeostasis, and suppresses tumor growth in subcutaneous xenograft models. SKLB06489 can be used for the research of triple-negative breast cancer (TNBC).
    SKLB06489
  • HY-113786
    EZH2-IN-21
    		Inhibitor
    EZH2-IN-21 is a potent inhibitor of the histone lysine methyltransferase enhancer of zeste homologue 2 (EZH2) with anticancer activity. EZH2-IN-21 is competitive with the cofactor SAM and noncompetitive with peptide or nucleosome substrates.
    EZH2-IN-21
  • HY-149005
    PRMT5-IN-19
    		Inhibitor
    PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research.
    PRMT5-IN-19
  • HY-181260
    PRMT5-MTA-IN-8
    		Inhibitor
    PRMT5-MTA-IN-8 is an orally active PRMT5-MTA complex inhibitor (IC50 = 4.4 nM). PRMT5-MTA-IN-8 inhibits the intracellular production of symmetric dimethylarginine (SDMA) as well as the proliferation of MTAP-deficient cells. PRMT5-MTA-IN-8 exerts antitumor efficacy by inhibiting PRMT5, reducing SDMA levels and inducing tumor cell apoptosis in mouse models of triple-negative breast cancer. PRMT5-MTA-IN-8 can be used in research related to cancers such as triple-negative breast cancer.
    PRMT5-MTA-IN-8
  • HY-116708
    DCE_254
    		Inhibitor
    DCE_254 is an EZH2 inhibitor (IC50=11 μM) that also exhibits significant antiproliferative activity against lymphoma cell lines. DCE_254 inhibits the development of hypermethylation-related cancers by inhibiting the SAM-mediated methyl transfer process (IC50=10.3 μM).
    DCE_254
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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