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Isoforms Recommended: EZH2
Results for "

EZH2,

" in MedChemExpress (MCE) Product Catalog:

87

Inhibitors & Agonists

2

Fluorescent Dye

1

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1

Peptides

2

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2

Antibodies

3

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-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-A0298

    Histone Methyltransferase Cancer
    EZH2-IN-2 is a EZH2 inhibitor extracted from patent WO2018133795A1, Compound Example 69, with an IC50 of 64 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity .
    EZH2-IN-2
  • 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-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-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-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-139150

    Histone Methyltransferase Cancer
    EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity .
    EZH2-IN-4
  • 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-163741

    Histone Methyltransferase Cancer
    EZH2-IN-19 (conpound N40) is a potent inhibitor of enhancer of zeste homolog 2 (EZH2) WT, with the IC50 of 0.32 nM. EZH2-IN-19 plays an important role in cancer research .
    EZH2-IN-19
  • HY-113786

    Histone Methyltransferase Cancer
    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-122595

    Histone Methyltransferase Cancer
    EZH2-IN-1 (compound 3) is a selective and SAM-competitive EZH2 and EZH1 inhibitor with an IC50s of 32 nM, 197 nM and 213 nM for EZH2wt, EZH2 Y641N mutant and EZH1, respectively. EZH2-IN-1 reduces bulk H3K27me3 and H3K27me2 levels. EZH2-IN-1 has the potential for diffuse large B cell lymphoma research .
    EZH2-IN-1
  • HY-161419

    Histone Methyltransferase Cancer
    EZH2-IN-18 (compound 9e) is a potent inhibitor of enhancer of zeste homologue 2 (EZH2 WT) , 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-153191

    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-144096

    Histone Methyltransferase Cancer
    EZH2-IN-11 is a potent inhibitor of E2HZ. The oncogenic activities of EZH2 have been shown by a number of studies in various different cancer types. EZH2-IN-11 has the potential for the research of cancer diseases (extracted from patent WO2019204490A1, compound 17) .
    EZH2-IN-11
  • 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-163288

    Histone Methyltransferase HSP Apoptosis Cancer
    EZH2/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) .
    EZH2/HSP90-IN-29
  • HY-144094

    Histone Methyltransferase Cancer
    EZH2-IN-9 is a potent inhibitor of EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH2-IN-9 has the potential for the research of cancer diseases (extracted from patent WO2021180235A1, compound 17) .
    EZH2-IN-9
  • HY-143616

    Histone Methyltransferase Cancer
    EZH2-IN-7 is a potent inhibitor of EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH2-IN-7 has the potential for the research of cancer diseases (extracted from patent WO2021129629A1, compound 259) .
    EZH2-IN-7
  • 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-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-157164

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-2 (compound E-3P-MDM2), an EZH2 inhibitor, is a PROTAC composed of Tazemetostat (EPZ6438) and an E3 ligase system ligand. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner, inhibits the expression of H3K27me3, and simultaneously degrades EED and SUZ12 proteins without affecting their mRNA levels. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity .
    PROTAC EZH2 Degrader-2
  • HY-168131

    Histone Methyltransferase Apoptosis Cancer
    PROTAC EZH2 Degrader-3 (compound ZJ-20) is a EZH2 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-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-156292

    Histone Methyltransferase Cancer
    IHMT-EZH2-426 (compound 38) is a potent and covalent EZH2 degrader with IC50s of 1.3 nM, 1.2 nM, and 1.7-3.5 nM against EZH2 wild-type, EZH2-A687V, and EZH2-Y641F/Y641N/Y641S, respectively. IHMT-EZH2-426 exhibits potent antiproliferation effects against both B-cell lymphoma and triple negative breast cancer (TNBC) cell lines by reducing the levels of H3K27me3 and EZH2 .
    IHMT-EZH2-426
  • 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-132885

    PARP Histone Methyltransferase Cancer
    PARP/EZH2-IN-1 is a first-in-class dual PARP (IC50 6.87 nM) and EZH2 (IC50 36.51 nM) inhibitor for triple-negative breast cancer with wild-type BRCA.
    PARP/EZH2-IN-1
  • HY-15573

    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-N5024
    Gambogenic acid
    1 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-144330

    Histone Methyltransferase Cancer
    TDI-6118 (Compound 5) is a potent inhibitor of EZH2. EZH2-IN-12 has the potential for the research of central nervous system malignancies .
    TDI-6118
  • HY-148333
    MS177
    1 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-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-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-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-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-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-154854

    Histone Methyltransferase Cancer
    BBDDL2059 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 .
    BBDDL2059
  • HY-13803
    Tazemetostat
    55+ 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-134899

    Histone Methyltransferase Cancer
    CPI-1328 is an EZH2 inhibitor with a Ki value of 63 fM.
    CPI-1328
  • HY-101571A

    Epigenetic Reader Domain Histone Methyltransferase Cancer
    PF-06821497 (compound 23a) is a potent, selective and orally active Enhancer of Zeste Homolog 2 (EZH2) inhibitor, with a Ki value <0.1 nM against mutant Y641N EZH2. Exhibits robust tumor growth inhibition .
    PF-06821497
  • 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-13803R

    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-13500
    GSK343
    20+ Cited Publications

    Histone Methyltransferase Autophagy Cancer
    GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.
    GSK343
  • HY-156615

    Histone Methyltransferase Cancer
    Igermetostat is EZH2 inhibitor, used in cancer research in vivo and in vitro .
    Igermetostat
  • 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-103682A

    Histone Methyltransferase Cancer
    PF-06726304 acetate is a potent and selective EZH2 inhibitor. PF-06726304 acetate inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 acetate displays robust antitumor growth activity .
    PF-06726304 acetate
  • HY-111085

    Histone Methyltransferase Cancer
    CPI-905 is a potent, selective, and cell-active EZH2 inhibitor .
    CPI-905
  • HY-117540

    Others Cancer
    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-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-133129
    MS1943
    1 Publications Verification

    Histone Methyltransferase Apoptosis Cancer
    MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines. MS1943 effectively blocks proliferation of multiple TNBC and other cancer cell lines .
    MS1943

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