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-141566
    EZH2-IN-5
    		Inhibitor
    EZH2-IN-5 is a potent EZH2 inhibitor with IC50 values of 1.52 nM and 4.07 nM for wild-type and mutant Tyr641 EZH2, respectively.
    EZH2-IN-5
  • HY-144187
    PRMT5-IN-16
    		Inhibitor
    PRMT5-IN-16 (Compound 20) 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-16
  • HY-181413
    PROTAC EZH2 Degrader-44
    		Degrader
    PROTAC EZH2 Degrader-44 (compound 60) is a highly efficient PROTAC degrader targeting the EZH2-PRC2 complex. By recruiting the CRBN E3 ligase and relying on the proteasome system, PROTAC EZH2 Degrader-44 simultaneously induces the degradation of core components EZH2, SUZ12 and EED, thereby significantly reducing the levels of H3K27me3 and CARM1. PROTAC EZH2 Degrader-44 exerts antiproliferative effects through a dual mechanism: on the one hand, it triggers mitochondrial dysfunction leading to decreased membrane potential; on the other hand, it strongly promotes apoptosis by regulating Bcl-2 family proteins (upregulating Bax, Caspase-3 and PARP, and downregulating Bcl-2). PROTAC EZH2 Degrader-44 exhibits only extremely low cytotoxicity in human normal mammary epithelial, liver and kidney cells, showing a favorable safety window. PROTAC EZH2 Degrader-44 is an ideal tool molecule for exploring the mechanisms of targeted therapy for triple-negative breast cancer.
    PROTAC EZH2 Degrader-44
  • HY-181522
    PRMT5 ligand 3
    		Ligand
    PRMT5 ligand 3 (Compound S19) is a PRMT5 ligand that can be used for the synthesis of PROTACs, such as RAPRMT5 (HY-181521).
    PRMT5 ligand 3
  • HY-117540
    ZLD10A
    ZLD10A is a highly potent and selective EZH2 inhibitor with the activity of inhibiting H3K27 methylation. ZLD10A can inhibit wild-type and mutant EZH2 with nanomolar potency and has more than 1000-fold selectivity for the other 10 histone methyltransferases. ZLD10A inhibited cell proliferation of DLBCL cell lines in a concentration- and time-dependent manner, showing a potential antiproliferative effect. ZLD10A can be used in the study of EZH2 mutant lymphomas.
    ZLD10A
  • HY-125090
    PHA-680626
    		Inhibitor
    PHA-680626 is an effective inhibitor of the interaction between Aurora-A and N-Myc. PHA-680626 inhibits kinase activity of AURKA and Bcr-Abl, and induces N-Myc degradation. PHA-680626 decreases phosphorylation of CrkL and histone H3. PHA-680626 shows anti-proliferative and pro-apoptotic activity on Imatinib (HY-15463)-resistant chronic myeloid leukemia cell lines and primary CD34+ cells.
    PHA-680626
  • HY-181324
    PROTAC EZH2 Degrader-23
    PROTAC EZH2 Degrader-23 (compound 8) is a PROTAC protein degrader targeting EZH2 with a target IC50 of 30.00 nM. PROTAC EZH2 Degrader-23 inhibits EZH2 methyltransferase activity via interaction with the EZH2 SET domain.
    PROTAC EZH2 Degrader-23
  • HY-176701
    PRMT5-MTA-IN-4
    		Inhibitor
    PRMT5-MTA-IN-4 (Compound 30) is a potent irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50=8 nM). PRMT5-MTA-IN-4 blocks arginine methylation, inhibiting ribosomal RNA processing and cell cycle-related protein expression. PRMT5-MTA-IN-4 exhibits antiproliferative activity in multiple tumor cell lines (e.g., IC50=0.3 μM in DLD-1 cells). PRMT5-MTA-IN-4 is promising for research of hematological malignancies, such as acute myeloid leukemia, diffuse large B-cell lymphoma.
    PRMT5-MTA-IN-4
  • HY-15650A
    SGC0946 TFA
    		Inhibitor
    SGC0946 TFA is a selective DOT1L inhibitor with an IC50 value of 0.3 nM. By inhibiting DOT1L, SGC0946 TFA can induce G1 phase arrest, suppress cell self-renewal and metastatic potential, and induce cell differentiation in cancer cells. SGC0946 TFA can be used in the research of tumors such as leukemia and breast cancer, and also serves as a probe to further investigate the cellular mechanisms of DOT1L in normal and diseased cells.
    SGC0946 TFA
  • HY-P2025
    JMV 236
    JMV 236 is a cholecystokinin antagonist with appetite-suppressing activity. JMV 236 affects the regulation of food intake through the interaction of the intestinal endogenous peptide PrRP and the CCK1 receptor. The administration of JMV 236 activates PrRP neurons located in the NTS, thereby enhancing its appetite-suppressing effect. JMV 236 has significant effects on areas of the central nervous system associated with food intake, especially during states of starvation.
    JMV 236
  • HY-179500
    EZH2 ligand-Linker Conjugate 1
    EZH2 ligand-Linker Conjugate 1 is a target protein ligand-lnker conjugate that incorporates a target protein ligand for EZH2. EZH2 ligand-Linker Conjugate 1 can be used for the synthesis of PROTAC EZH2 Degrader-9 (HY-179499).
    EZH2 ligand-Linker Conjugate 1
  • HY-12707C
    Piribedil hydrochloride
    		Inhibitor
    Piribedil hydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil hydrochloride is also a α2-adrenoceptors antagonist. Piribedil hydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil hydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers.
    Piribedil hydrochloride
  • HY-181790
    DOT1L ligand-2
    		Ligand
    DOT1L ligand-2 (Compound 52) is a DOT1L ligand. DOT1L ligand-2 acts as a Ligand for Target Protein for PROTAC, which is used to develop and design degraders of PROTAC DOT1L, such as DOT1L808 (HY-181789). DOT1L ligand-2 is applicable to research related to MLL-rearranged leukemia.
    DOT1L ligand-2
  • HY-155154
    PRMT4-IN-2
    		Inhibitor
    PRMT4-IN-2 (compound 55) is a pan-inhibitor of protein arginine methyltransferase (PRMT) with IC50s of 92 nM (PRMT4), 436 nM (PRMT6), 460 nM (PRMT1), 823 nM ( PRMT8), 1.386 μM (PRMT3).
    PRMT4-IN-2
  • HY-178694
    DC-PRC2in-01
    		Inhibitor
    DC-PRC2in-01 is a potent EZH2-EED interaction inhibitor with an IC50 of 4.21 μM and a Kd of 4.56 μM. DC-PRC2in-01 disrupts the EZH2-EED interaction, leading to degradation of PRC2 core proteins and decrease of H3K27me3 levels, inhibition of PRC2-driven lymphoma cell proliferation, and cell cycle arrest. DC-PRC2in-01 can be used for the research of PRC2-related cancers, such as Diffuse Large B-cell Lymphoma (DLBCL) and follicular lymphoma (FL).
    DC-PRC2in-01
  • HY-181319
    PROTAC EZH2 Degrader-21
    		Degrader
    PROTAC EZH2 Degrader-21 is an EZH2 degrader developed based on PROTAC technology. PROTAC EZH2 Degrader-21 induces the degradation of the target protein EZH2 via specific recruitment of the cIAP E3 ligase. PROTAC EZH2 Degrader-21 exhibits significant inhibitory activity in a variety of lymphoma cell lines. PROTAC EZH2 Degrader-21 can be used for research on the pathogenesis of lymphoma.
    PROTAC EZH2 Degrader-21
  • HY-P10948
    CS-VIP 8
    		Inhibitor
    CS-VIP 8 is a selective allosteric WDR5 protein inhibitor (Ki= 0.008 μM). CS-VIP 8 induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 is promising for research of hematological diseases such as leukemia.
    CS-VIP 8
  • HY-155020
    Antitumor agent-101
    		Inhibitor
    Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model.
    Antitumor agent-101
  • HY-174397
    EED-IN-3
    		Inhibitor
    EED-IN-3 is an orally active EED inhibitor. EED-IN-3 effectively inhibits PRC2 by binding to EED (IC50 = 0.62 μM for EED) and downregulates H3K27me3. EED-IN-3 can efficiently and selectively inhibit PC3 cells with the IC50 of 3.69 μΜ and could significantly suppress colony formation and migration. EED-IN-3 can be used for research on prostate cancer.
    EED-IN-3
  • HY-181332
    PROTAC EZH2 Degrader-37
    		Degrader
    PROTAC EZH2 Degrader-37 (compound 16) is a PROTAC protein degrader targeting EZH2 with a target IC50 of 144 nM. PROTAC EZH2 Degrader-37 is applicable to lymphoma-related research.
    PROTAC EZH2 Degrader-37
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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