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Isoforms Recommended: EZH2
Results for "

EZH2

" in MedChemExpress (MCE) Product Catalog:

165

Inhibitors & Agonists

2

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3

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2

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3

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1

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1

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4

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4

Click Chemistry

3

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1

GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13803
    Tazemetostat
    85+ Cited Publications

    EPZ-6438; E-7438

    Histone Methyltransferase Apoptosis Cancer
    Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells .
    Tazemetostat
  • HY-13500
    GSK343
    30+ Cited Publications

    Histone Methyltransferase Autophagy Cancer
    GSK343, a chemical probe, is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.
    GSK343
  • HY-145602

    CPI-0209

    Histone Methyltransferase Cancer
    Tulmimetostat (CPI-0209) is an orally active EZH1/EZH2 inhibitor that targets and inhibits the EZH2 enzyme.Tulmimetostat has antitumor activity and is used in a variety of solid tumor studies [2] .
    Tulmimetostat
  • HY-133129
    MS1943
    4 Publications Verification

    HyT Histone Methyltransferase Apoptosis Inflammation/Immunology Cancer
    MS1943 is an orally active selective HyT degrader of EZH2 that effectively reduces EZH2 levels in cells. MS1943 has anticancer activity and exhibits cytotoxic effects in a variety of TNBC cells while sparing normal cells. In addition, MS1943 maintains high potency (IC50=120 nM) in inhibiting EZH2 methyltransferase activity and is highly selective for EZH2. (Structure Note: RED, EZH2 ligand (HY-148458); Blue, Hyt (HY-W001578)) .
    MS1943
  • HY-N5024
    Gambogenic acid
    2 Publications Verification

    Histone Methyltransferase Cancer
    Gambogenic acid is an active ingredient that can be isolated from gamboge. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination. Gambogenic acid can be used for the research of cancer [2].
    Gambogenic acid
  • HY-147525
    PROTAC EZH2 Degrader-1
    1 Publications Verification

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes .
    PROTAC EZH2 Degrader-1
  • HY-148333
    MS177
    3 Publications Verification

    PROTACs Histone Methyltransferase Apoptosis Cancer
    MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12 nM). MS177 effectively depletes both canonical EZH2-PRC2 and noncanonical EZH2-cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest .
    MS177
  • HY-153191
    EZH2-IN-15
    1 Publications Verification

    Histone Methyltransferase Cancer
    EZH2-IN-15 is a EZH2 inhibitor. EZH2-IN-15 has anti-tumor activity, and can be used for research of H3K27me3-dependent tumors .
    EZH2-IN-15
  • HY-148458

    Histone Methyltransferase Cancer
    EZH2-IN-14 is a selective EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 12 nM. EZH2-IN-14 inhibits the methyltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3). EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 .
    EZH2-IN-14
  • HY-147091

    Ligands for Target Protein for PROTAC Cancer
    Tazemetostat de(methyl morpholine)-COOH (compound 7) is a ligand for the PROTAC target protein EZH2, which can be used to synthesis of EZH2 degraders (PROTACs). EZH2 degraders have potent cell viability inhibition in diffuse large B-cell lymphoma (DLBCL) and other subtypes of lymphoma .
    Tazemetostat de(methyl morpholine)-COOH
  • HY-157164
    PROTAC EZH2 Degrader-2
    1 Publications Verification

    PROTACs Histone Methyltransferase Apoptosis Cancer
    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 .
    PROTAC EZH2 Degrader-2
  • HY-13803R

    EPZ-6438 (Standard); E-7438 (Standard)

    Reference Standards Histone Methyltransferase Apoptosis Cancer
    Tazemetostat (Standard) is the analytical standard of Tazemetostat. This product is intended for research and analytical applications. Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells .
    Tazemetostat (Standard)
  • HY-103682
    PF-06726304
    1 Publications Verification

    Histone Methyltransferase Cancer
    PF-06726304 is a potent and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 displays robust antitumor growth activity .
    PF-06726304
  • HY-A0298

    Histone Methyltransferase Cancer
    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 .
    EZH2-IN-2
  • HY-15573
    EI1
    2 Publications Verification

    KB-145943

    Histone Methyltransferase Apoptosis Cancer
    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.
    EI1
  • HY-101508

    Histone Methyltransferase Cancer
    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 .
    GNA002
  • HY-148334

    PROTACs Histone Methyltransferase Cancer
    MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader. MS8815 has inhibition activity for EZH2 with an IC50 value of 8.6 nM. MS8815 can be used for the research of triple-negative breast cancer (TNBC) .
    MS8815
  • HY-RS04619

    Small Interfering RNA (siRNA) Others

    EZH2 Human Pre-designed siRNA Set A contains three designed siRNAs for EZH2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    EZH2 Human Pre-designed siRNA Set A
    EZH2 Human Pre-designed siRNA Set A
  • HY-116804

    Histone Methyltransferase Cancer
    ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis .
    ZLD1039
  • HY-100846
    JQEZ5
    3 Publications Verification

    Histone Methyltransferase Cancer
    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 .
    JQEZ5
  • HY-144330

    Histone Methyltransferase Cancer
    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 .
    TDI-6118
  • HY-12856
    GSK503
    5+ Cited Publications

    Histone Methyltransferase Cancer
    GSK503 is a potent and specific inhibitor of EZH2 methyltransferase with Ki app values of 3 to 27 nM.
    GSK503
  • HY-168131

    PROTACs Histone Methyltransferase Apoptosis Cancer
    PROTAC EZH2 Degrader-3 (compound ZJ-20) is a EZH2 PROTAC degrader. PROTAC EZH2 Degrader-3 (5 μM, 24 h) not only potently inhibits the expression of EZH2 protein, but also had a strong inhibits effect on the expression levels of other subunits of PRC2 as well as H3k27me3 protein. PROTAC EZH2 Degrader-3 shows anti-proliferative activity and blocks the cell cycle in the G0-G1 phase and induces cell apoptosis((Blue: cereblon ligand Pomalidomide (HY-10984), Black: linker HY-W361751;Pink: EZH2 inhibitor Tazemetostat (HY-13803)) .
    PROTAC EZH2 Degrader-3
  • HY-RS04620

    Small Interfering RNA (siRNA) Others

    Ezh2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Ezh2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Ezh2 Mouse Pre-designed siRNA Set A
    Ezh2 Mouse Pre-designed siRNA Set A
  • HY-176165

    CDK Histone Methyltransferase Cancer
    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) .
    CDK9/EZH2-IN-1
  • HY-141566

    Histone Methyltransferase Cancer
    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-136188

    Histone Methyltransferase Cancer
    UNC2399, a biotinylated UNC1999, is a selective EZH2 inhibitor, maintaining high in vitro potency for EZH2, with an IC50 of 17 nM [2].
    UNC2399
  • HY-149726

    Histone Methyltransferase Cancer
    EZH2-IN-17 (compound 28) is a potent and orally active EZH2 inhibitor with an IC50 value of 0.95 nM. EZH2-IN-17 exhibits high anti-proliferation activity against different lymphoma cell lines including WSU-DLCL2, Pfeiffer and Karpas-422 (IC50 values of 2.36 nM, 1.73 nM, and 1.82 nM, respectively) .
    EZH2-IN-17
  • HY-D2274

    Fluorescent Dye Others
    EZH2-AF647 is a fluorescent probe derived from UNC2239 that improves receptor TR-FRET properties by using Alexa 647 dye .
    EZH2-AF647
  • HY-132885

    PARP Histone Methyltransferase Cancer
    PARP/EZH2-IN-1 is a first-in-class dual PARP-1/EZH2 inhibitor with IC50 values of 6.87 nM and 36.51 nM, respectively. PARP/EZH2-IN-1 induces autophagy in cancer cells and shows potent antiproliferative activity in BRCA wild-type triple-negative breast cancer cells .
    PARP/EZH2-IN-1
  • HY-174372

    Histone Methyltransferase Cancer
    EZH2-IN-23 (Compound 25) is an EZH2 inhibitor that exhibits potent enzymatic inhibition of the PRC2 complex (EZH2, EED, SUZ12, AEBP2, RbAp48) with a biochemical IC50 of 0.8 nM. EZH2-IN-23 inhibits H3K27 trimethylation in cellular assays, showing an IC50 of 40 nM. EZH2-IN-23 displays good rat PKproperties with 100 % oral bioavailability.
    EZH2-IN-23
  • HY-147230

    Histone Methyltransferase Cancer
    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 .
    EZH2-IN-13
  • HY-P2266

    Histone Methyltransferase Cancer
    SAH-EZH2, a stable EZH2 α-helical peptide, is an EZH2/EED interaction inhibitor. SAH-EZH2 targets native embryonic ectoderm development (EED), disturbs its interactions with EZH1 and EZH2, and selectively decreases trimethylation of H3K27 .
    SAH-EZH2
  • HY-179386

    PARP Histone Methyltransferase Apoptosis Pyroptosis Necroptosis Reactive Oxygen Species (ROS) PANoptosis Cancer
    PARP1/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 .
    PARP1/EZH2-IN-1
  • HY-156292

    Histone Methyltransferase Cancer
    IHMT-EZH2-426 (compound 38) is an effective covalent EZH2 degrader, with IC50 values of 1.3 nM, 1.2 nM, and 1.7-3.5 nM for EZH2 wild type, EZH2-A687V, and EZH2-Y641F/Y641N/Y641S, respectively. IHMT-EZH2-426 reduces H3K27me3 and EZH2 levels and shows effective anti-proliferative effects in B-cell lymphoma and TNBC cell lines.
    IHMT-EZH2-426
  • HY-144882

    Histone Methyltransferase Inflammation/Immunology Cancer
    (R)-HH2853 is a mutant EZH2 inhibitor with an IC50 of <100 nM for EZH2-Y641F. (R)-HH2853 can be used for cancer and autoimmune diseases (WO2018045971A1; compound 201) .
    (R)-HH2853
  • HY-16986B
    EPZ011989 hydrochloride
    3 Publications Verification

    Histone Methyltransferase Cancer
    EPZ011989 hydrochloride is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor, with a Ki value of <3 nM. EPZ011989 shows anti-tumor activity. EPZ011989 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups .
    EPZ011989 hydrochloride
  • HY-122936

    Histone Methyltransferase Keap1-Nrf2 Sirtuin Cardiovascular Disease Cancer
    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 [2].
    Tanshindiol C
  • HY-149463

    Histone Methyltransferase Cancer
    EZH2-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 .
    EZH2-IN-16
  • HY-RS04621

    Small Interfering RNA (siRNA) Others

    Ezh2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Ezh2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Ezh2 Rat Pre-designed siRNA Set A
    Ezh2 Rat Pre-designed siRNA Set A
  • HY-161083

    PARP Histone Methyltransferase Cancer
    PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy .
    PARP/EZH2-IN-2
  • HY-181324

    PROTACs Histone Methyltransferase Cancer
    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-181333

    PROTACs Histone Methyltransferase Others
    PROTAC EZH2 Degrader-38 (Compound 17) is a EZH2 PROTAC degrader with an IC50 of 165.00 nM. PROTAC EZH2 Degrader-38 functionally inhibits the methyltransferase activity of EZH2 and competitively binds to the SAM-binding pocket of the EZH2 SET domain .
    PROTAC EZH2 Degrader-38
  • HY-181393

    Ligands for Target Protein for PROTAC Histone Methyltransferase Cancer
    EZH2 ligand-3, a EZH2 ligand, is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). EZH2 ligand-3 can be used for the synthesis of PROTAC EZH2 Degrader-35 (HY-181392) .
    EZH2 ligand-3
  • HY-181325

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-24 (compound 9) is an EZH2-targeting PROTAC with EZH2 methyltransferase inhibitory activity .
    PROTAC EZH2 Degrader-24
  • HY-181332

    PROTACs Histone Methyltransferase Cancer
    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
  • HY-181331

    PROTACs Histone Methyltransferase Others
    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-181334

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-39 (compound 18) is a PROTAC protein degrader targeting EZH2 with a target IC50 of 61.00 nM. PROTAC EZH2 Degrader-39 functionally inhibits EZH2 methyltransferase activity .
    PROTAC EZH2 Degrader-39
  • HY-181327

    PROTACs Histone Methyltransferase Others
    PROTAC EZH2 Degrader-26 (compound 11) is an EZH2 degrader developed based on PROTAC technology. PROTAC EZH2 Degrader-26 has an IC50 of 5.80 nM against EZH2. PROTAC EZH2 Degrader-26 exhibits micromolar-level enzyme inhibitory activity against EZH1, with an EZH1 IC50 of 0.06 μM .
    PROTAC EZH2 Degrader-26
  • HY-181309

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-15 (compound 5) is an EZH2-targeting PROTAC. PROTAC EZH2 Degrader-15 functionally inhibits EZH2 methyltransferase activity .
    PROTAC EZH2 Degrader-15

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