2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase
  5. EZH2 Isoform

EZH2

EZH2 is the catalytic methyltransferase subunit of the Polycomb Repressive Complex 2 (PRC2) and mediates transcriptional repression through trimethylation of histone H3 lysine 27 (H3K27me3), thereby regulating cell proliferation, differentiation, and developmental gene expression programs[1][2][3]. Mechanistically, PRC2-dependent H3K27 methylation establishes repressive chromatin states and cooperates with other epigenetic silencing pathways to maintain stable suppression of target genes[4][5]. Through this epigenetic mechanism, EZH2 controls critical biological processes including cell-cycle regulation, lineage commitment, and transcriptional programs linked to tissue homeostasis and disease development[2][6]. In disease contexts, aberrant EZH2 expression or activity is frequently associated with cancer progression, where enhanced H3K27me3-mediated repression contributes to tumor cell proliferation, survival, invasion, metastasis, and drug resistance[2][3][7][8]. Experimental studies further demonstrate that EZH2 silencing can inhibit tumor growth and metastatic dissemination while restoring expression of tumor-suppressive genes, supporting its functional role in oncogenic epigenetic regulation[7]. Compared with the related isoform EZH1, EZH2 is generally regarded as the dominant catalytic component driving PRC2 methyltransferase activity in proliferating cells and is therefore the principal focus of therapeutic targeting strategies directed at PRC2-dependent chromatin regulation[1][9]. For experimental applications, selective EZH2 inhibitors have become important tools for investigating PRC2 biology and epigenetic gene repression, and the clinical development of agents such as tazemetostat has validated EZH2 as a tractable target for mechanistic and translational research in cancer models[9][10][11].

References:

EZH2 관련 제품 (76):

Cat. No. 상품명 효과 Purity
  • HY-157844
    NUCC-0226272
    		Degrader 99.68%
    NUCC-0226272 is a potent PROTAC that targets EZH2 for degradation. NUCC-0226272 has anti-proliferative effect. NUCC-0226272 has the potential for cancer research.
  • HY-78694
    5-Bromo-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2-methylbenzamide
    		Ligand 98.22%
    5-Bromo-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2-methylbenzamide is a drug intermediate for synthesis of various active compounds.
  • HY-100846
    JQEZ5
    		Inhibitor 98.14%
    JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitively inhibits polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects.
  • HY-12856
    GSK503
    		Inhibitor 99.52%
    GSK503 is a potent and specific inhibitor of EZH2 methyltransferase with Kiapp values of 3 to 27 nM.
  • HY-157164
    PROTAC EZH2 Degrader-2
    		Degrader 98.77%
    PROTAC EZH2 Degrader-2 is a PROTAC EZH2 inhibitor. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner. PROTAC EZH2 Degrader-2 induces apoptosis and reduces mitochondrial membrane potential in SU-DHL-6 cells. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity.
  • HY-15573
    EI1
    		Inhibitor 98.84%
    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.
  • 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.
  • HY-162384
    EPIC-0628
    		Inhibitor 98.93%
    EPIC-0628 is an inhibitor of the HOTAIR-EZH2 interaction and promotes ATF3 expression. The long noncoding RNA HOTAIR has been found to regulate glioblastoma (GBM) progression and mediate DNA damage repair (DDR) by interacting with the catalytic subunit EZH2 of PRC2. EPIC-0628 also inhibits the ATF3-p38-E2F1 DDR pathway to inhibit the HR pathway and upregulates CDKN1A (p21) expression, causing cell cycle arrest. EPIC-0628 also synergizes with Temozolomide (TMZ) (HY-17364) to enhance its in vivo potency.
  • HY-141877B
    MS4322 (isomer)
    		99.87%
    MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )).
  • HY-147230
    EZH2-IN-13
    		Inhibitor 99.72%
    EZH2-IN-13 is a potent EZH2 inhibitor, for details please refer to compound 73 in patent WO2017139404. EZH2-IN-13 can be used to study cancers or precancerous lesions associated with EZH2 activity.
  • HY-144330
    TDI-6118
    		Inhibitor 99.08%
    TDI-6118 (Compound 5) is a potent brain-penetrant inhibitor of EZH2. EZH2-IN-12 has the potential for the research of central nervous system malignancies.
  • HY-A0298
    EZH2-IN-2
    		Inhibitor 98.51%
    EZH2-IN-2 (Example 69) is a EZH2 inhibitor with an IC50 and a TR-FRET IC50 of 64 nM and 20 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity.
  • HY-101508
    GNA002
    		Inhibitor 98.02%
    GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes.
  • HY-176165
    CDK9/EZH2-IN-1
    		Inhibitor 99.08%
    CDK9/EZH2-IN-1 (Compound D16) is a CDK9/EZH2 dual-target inhibitor (IC50: 83.9/108.6 nM). CDK9/EZH2-IN-1 induces apoptosis and DNA double-strand breaks (DSBs). CDK9/EZH2-IN-1 inhibits the proliferation activity of MKN45, MDA-MB-453 and SW620 cancer cells (IC50 values are 136.3, 171.3 and 315.7 nM, respectively).
  • HY-131246
    DM-01
    		Inhibitor 98.05%
    DM-01 is a powerful and selective EZH2 inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors.
  • HY-119198
    NSC745885
    		Inhibitor 98.0%
    NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers.
  • HY-146999
    YM458
    		Inhibitor 99.16%
    YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer.
  • HY-111418
    EBI-2511
    		Inhibitor 98.67%
    EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC50 of 6 nM in Pfeffiera cell lines, respectively.
  • HY-136188
    UNC2399
    		Inhibitor 99.16%
    UNC2399, a biotinylated UNC1999, is a selective EZH2 inhibitor, maintaining high in vitro potency for EZH2, with an IC50 of 17 nM.
  • HY-122936
    Tanshindiol C
    		Inhibitor 98.47%
    Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research.
Cat. No. 상품명 / Synonyms Application Reactivity