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][1]. 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][6]. 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[6]. 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][7]. 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[7][8][9].
References:
- [1]. Tan JZ, et al. EZH2: biology, disease, and structure-based drug discovery. Acta Pharmacol Sin. 2014 Feb;35(2):161-74. [Content Brief]
- [2]. Gan L, et al. Epigenetic regulation of cancer progression by EZH2: from biological insights to therapeutic potential. Biomark Res. 2018 Mar 9;6:10. [Content Brief]
- [3]. Saijo N. Present status and problems on molecular targeted therapy of cancer. Cancer Res Treat. 2012 Mar;44(1):1-10. doi: 10.4143/crt.2012.44.1.1. Epub 2012 Mar 31. PMID: 22500155; PMCID: PMC3322195. et al. Present status and problems on molecular targeted therapy of cancer. Cancer Res Treat. 2012 Mar;44(1):1-10. [Content Brief]
- [4]. Muntean AG, et al. Epigenetic dysregulation in cancer. Am J Pathol. 2009 Oct;175(4):1353-61. [Content Brief]
- [5]. Peter EK, et al. A Hybrid Hamiltonian for the Accelerated Sampling along Experimental Restraints. Int J Mol Sci. 2019 Jan 16;20(2):370. [Content Brief]
- [6]. Lv YF, et al. Enhancer of zeste homolog 2 silencing inhibits tumor growth and lung metastasis in osteosarcoma. Sci Rep. 2015 Aug 12;5:12999. [Content Brief]
- [7]. Shi Y, et al. Structure of the PRC2 complex and application to drug discovery. Acta Pharmacol Sin. 2017 Jul;38(7):963-976. [Content Brief]
- [8]. Xia J, et al. Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects. J Med Chem. 2022 May 26;65(10):7016-7043. [Content Brief]
- [9]. Straining R, et al. Tazemetostat: EZH2 Inhibitor. J Adv Pract Oncol. 2022 Mar;13(2):158-163. [Content Brief]
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EZH2 Related Products (85)
Related Products (85)
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Antibodies (31)
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EPZ011989 trifluoroacetate
0 ImagesCat. No.: HY-16986ACAS No.: 1598383-41-5EPZ-011989 trifluoroacetate is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. EPZ-011989 trifluoroacetate can be used for the research of various cancers. EPZ011989 (trifluoroacetate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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(S)-HH2853
0 ImagesCat. No.: HY-144881CAS No.: 2202678-05-3(S)-HH2853 (compound 200), a PYRIDINO five membered aromatic ring compound, is a potent EZH1/2 dual inhibitor with an IC50 of <100 nM for EZH2_Y641F. (S)-HH2853 has the potential to be used in the research of anti-tumor or autoimmune diseases.
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(R)-HH2853
0 ImagesCat. No.: HY-144882CAS No.: 2202678-06-4
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CPI-1328
0 ImagesCat. No.: HY-134899CAS No.: 2390367-27-6CPI-1328 is an EZH2 inhibitor with a Ki value of 63 fM.
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PF-06726304 acetate
0 ImagesCat. No.: HY-103682ACAS No.: 2080306-28-9
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3-Deazaneplanocin A hydrochloride (GMP)
0 ImagesCat. No.: HY-12186GCAS No.: 120964-45-6Synonyms: DZNep hydrochloride (GMP); NSC 617989 hydrochloride (GMP); 3-Deazaneplanocin hydrochloride (GMP)3-Deazaneplanocin A (DZNep) hydrochloride (GMP) is 3-Deazaneplanocin A hydrochloride (HY-12186) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 3-Deazaneplanocin A hydrochloride is a potent histone methyltransferase EZH2 inhibitor.
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IHMT-EZH2-426
0 ImagesCat. No.: HY-156292CAS No.: 3018914-66-1IHMT-EZH2-426 is an orally active and selective EZH2 degrader. IHMT-EZH2-426 forms a covalent bond with Cys663 of EZH2, inhibits its catalytic activity, and reduces the protein levels of EZH2 as well as the level of H3K27me3. IHMT-EZH2-426 acts as an antiproliferative agent against B-cell lymphoma and triple-negative breast cancer cells, and also exhibits anti-tumor related activity in Pfeiffer and MDA‑MB‑231 xenograft models. IHMT-EZH2-426 can be used in studies related to B-cell lymphoma and triple-negative breast cancer.
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BBDDL2059
0 ImagesCat. No.: HY-154854CAS No.: 2691174-27-1BBDDL2059 is a selective covalent inhibitor of histone methyltransferase EZH2 with an IC50 of 1.5 nM for EZH2-Y641F. BBDDL2059 inhibits lymphoma cell growth at nanomolar concentrations and can be used for anticancer research.
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PARP1/EZH2-IN-1
0 ImagesCat. No.: HY-179386PARP1/EZH2-IN-1 is a selective PARP1 and EZH2 dual inhibitor. PARP1/EZH2-IN-1 has IC50s of 28 nM, 414 nM and 74 nM for PARP1, PARP2 and EZH2, respectively. PARP1/EZH2-IN-1 inhibits the proliferation and migration of TNBC cells (triple-negative breast Cancer cells). PARP1/EZH2-IN-1 induces PANoptosis (Apoptosis, Pyroptosis and Necroptosis), increases the level of reactive oxygen species (ROS), and activates related inflammatory pathways. PARP1/EZH2-IN-1 can be used in triple-negative breast cancer research.
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EZH2/HSP90-IN-29
0 ImagesCat. No.: HY-163288CAS No.: 3033571-35-3EZH2/HSP90-IN-29 is a dual inhibitor for EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively. EZH2/HSP90-IN-29 increases apoptosis/necrosis-related gene expression, induces cell cycle arrest at M phase and inhibits reactive oxygen species (ROS) catabolism pathway. EZH2/HSP90-IN-29 is able to cross the blood-brain-barrier (BBB).
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EZH2-IN-16
0 ImagesCat. No.: HY-149463CAS No.: 2238820-26-1EZH2-IN-16 (Compound 24) is an inhibitor for histone methyltransferase (EZH2). EZH2-IN-16 inhibits EZH2 and EZH2 Y641F, with IC50 of 37.6 and 79.1 nM. EZH2-IN-16 inhibits proliferation of WSU-DLCL2, with GI50 of 0.2 μM.
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EZH2 ligand-1
0 ImagesCat. No.: HY-179351CAS No.: 2641602-26-6
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PROTAC EZH2 Degrader-3
0 ImagesCat. No.: HY-168131CAS No.: 3098718-46-5PROTAC EZH2 Degrader-3 is a EZH2 PROTAC degrader. PROTAC EZH2 Degrader-3 induces the global degradation of the PRC2 complex (including EZH2, SUZ12, EED, RbAp48) via the ubiquitin-proteasome pathway and downregulates H3K27me3 levels. PROTAC EZH2 Degrader-3 inhibits cancer cell proliferation and induces their apoptosis. PROTAC EZH2 Degrader-3 can be used in research related to lymphoblastoma and diffuse large B-cell lymphoma.
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YM1240
0 ImagesCat. No.: HY-184270YM1240 is an orally active dual EZH2/HDAC inhibitor with human EZH2 IC50 0.342 μM and human HDAC IC50 0.12 μM. YM1240 inhibits EZH2 pathway to reduce H3K27me3 levels, inhibits HDAC pathway to increase H3K9ac and H4ac levels. YM1240 suppresses proliferation, induces apoptosis, induces cell cycle arrest in lymphoma cells. YM1240 exhibits antitumor efficacy in lymphoma xenograft models. YM1240 can be used for the research of lymphoma.
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HDACs/EZH2-IN-1
0 ImagesCat. No.: HY-169400HDACs/EZH2-IN-1 (Compound 22a) is a HDACs/EZH2 inhibitor (EZH2 Y641N inhibition rate at 50 nM: 98%), with selective inhibition against HDAC1 and HDAC6 (IC50: 0.23 μM and 0.07 μM, respectively). HDACs/EZH2-IN-1 exerts a antiproliferative effect on diffuse large B-cell lymphoma cells harboring an EZH2 mutation and on various acute myeloid leukemia cells. HDACs/EZH2-IN-1 has the ability to induce cell differentiation and Apoptosis.
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PROTAC EZH2 Degrader-9
0 ImagesCat. No.: HY-179499CAS No.: 2978620-84-5PROTAC EZH2 Degrader-9 is orally active EZH2 PROTAC degrader degrading EZH2 via the ubiquitin-proteasome pathway. PROTAC EZH2 Degrader-9 downregulates PRC2 core subunits and potent inhibition of H3K27me3 without affecting common CRBN neosubstrates while it was selective over GSp'T1 and ikZF1/3. PROTAC EZH2 Degrader-9 exhibits potent antiproliferative activity against multiple cancer cell lines by inducing cell cycle and apoptosis. PROTAC EZH2 Degrader-9 reverses PRC2-mediated gene silencing and inhibiting EZH2 non-catalytic target gene activation. PROTAC EZH2 Degrader-9 can be used for leukemia, lymphoma, and non-small cell lung cancer research.
