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Results for "

EZH2 inhibitor

" in MedChemExpress (MCE) Product Catalog:

60

Inhibitors & Agonists

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Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-148458
    EZH2-IN-14

    		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-116804
    ZLD1039

    		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-149726
    EZH2-IN-17

    		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-154854
    BBDDL2059

    		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-149463
    EZH2-IN-16

    		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-147230
    EZH2-IN-13

    		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-144330
    EZH2-IN-12

    		Histone Methyltransferase Cancer
    EZH2-IN-12 (Compound 5) is a potent inhibitor of EZH2. EZH2-IN-12 has the potential for the research of central nervous system malignancies .
    EZH2-IN-12
  • HY-A0298
    EZH2-IN-2

    		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-P2266
    SAH-EZH2

    		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-139150
    EZH2-IN-4

    		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
    EZH2-IN-5

    		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-161419
    EZH2-IN-18

    		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-122595
    EZH2-IN-1

    		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-15573
    EI1

    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-153191
    EZH2-IN-15

    		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-163288
    EZH2/HSP90-IN-29

    		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-161083
    PARP/EZH2-IN-2

    		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-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 .
    Gambogenic acid
  • HY-148333
    MS177

    		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-144096
    EZH2-IN-11

    		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-136188
    UNC2399

    		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 .
    UNC2399
  • HY-157164
    PROTAC EZH2 Degrader-2

    		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-144094
    EZH2-IN-9

    		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
    EZH2-IN-7

    		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-145602
    Tulmimetostat

    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 .
    Tulmimetostat
  • HY-132885
    PARP/EZH2-IN-1

    		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-101508
    GNA002

    		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-13803
    Tazemetostat
    50+ 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-144882
    (R)-HH2853

    		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-134899
    CPI-1328

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

    		Histone Methyltransferase Cancer
    Igermetostat is EZH2 inhibitor, used in cancer research in vivo and in vitro .
    Igermetostat
  • HY-101571A
    PF-06821497

    		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-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
    PF-06726304 acetate

    		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
    CPI-905

    		Histone Methyltransferase Cancer
    CPI-905 is a potent, selective, and cell-active EZH2 inhibitor .
    CPI-905
  • 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-13470
    GSK126
    Maximum Cited Publications
    58 Publications Verification

    GSK2816126A

    		 Histone Methyltransferase Cancer
    GSK126 (GSK2816126A) is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC50 of 9.9 nM .
    GSK126
  • HY-162250
    MS8847

    		PROTACs Histone Methyltransferase Cancer
    MS8847 is a highly potent EZH2 PROTAC degrader that recruits the E3 ligase von Hippel-Lindau (VHL). MS8847 potently degrades EZH2 in a ubiquitin-proteasome system-dependent manner. MS8847 effectively inhibits the growth of acute myeloid leukemia (AML) and triple-negative breast cancer (TNBC) cells .
    MS8847
  • HY-111418
    EBI-2511

    		Histone Methyltransferase Cancer
    EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC50 of 6 nM in Pfeffiera cell lines, respectively.
    EBI-2511
  • HY-144904
    MC4343

    		HDAC Cancer
    MC4343 is a potent and dual inhibitor of EZH2 and histone deacetylase. MC4343 has the potential for the research of cancer disease.
    MC4343
  • HY-15646
    UNC1999
    5+ Cited Publications

    		 Histone Methyltransferase Autophagy Cancer
    UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH2/1 with IC50s of <10 nM and 45 nM, repectively.
    UNC1999
  • HY-101512
    A-395

    		Histone Methyltransferase Cancer
    A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM .
    A-395
  • HY-16986
    EPZ011989
    2 Publications Verification

    		 Histone Methyltransferase Cancer
    EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ011989 shows robust methyl mark inhibition and anti-tumor activity. EPZ011989 can be used for the research of various cancers . 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
  • HY-15555
    EPZ005687
    5 Publications Verification

    		 Histone Methyltransferase Cancer
    EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, and has 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
    EPZ005687
  • HY-16986A
    EPZ011989 trifluoroacetate
    2 Publications Verification

    		 Histone Methyltransferase Cancer
    EPZ-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.
    EPZ011989 trifluoroacetate
  • 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-10442
    3-Deazaneplanocin A
    20+ Cited Publications

    DZNep; 3-Deazaneplanocin

    		 Histone Methyltransferase Orthopoxvirus Infection Cancer
    3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor . 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity .
    3-Deazaneplanocin A
  • HY-160765
    WNTinib

    APS-8-100-2

    		 Wnt Apoptosis Cancer
    WNTinib (APS-8-100-2) is a multi-kinase inhibitor that selectively antagonizes β-catenin (CTNNB1) mutated hepatocellular carcinoma (HCC). WNTinib downregulates oncogenicWntsignaling by inhibiting KIT/MAPK and downstream EZH2 activation .
    WNTinib
  • HY-144881
    (S)-HH2853

    		Histone Methyltransferase Inflammation/Immunology Cancer
    (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 .
    (S)-HH2853

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