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EZH2+inhibitor

" in MedChemExpress (MCE) Product Catalog:

43

Inhibitors & Agonists

1

Fluorescent Dyes

1

Biochemical Assay Reagents

1

GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13803
    Tazemetostat
    Maximum Cited Publications
    89 Publications Verification

    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-10442
    3-Deazaneplanocin A
    30+ Cited Publications

    DZNep; 3-Deazaneplanocin

    		 Histone Methyltransferase S-adenosylhomocysteine hydrolase (SAHH) Orthopoxvirus Infection Metabolic Disease Inflammation/Immunology Cancer
    3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor [2]. 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity .
    3-Deazaneplanocin A
  • 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
    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 [2] .
    Tulmimetostat
  • HY-12186
    3-Deazaneplanocin A hydrochloride
    30+ Cited Publications

    DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride

    		 Histone Methyltransferase S-adenosylhomocysteine hydrolase (SAHH) Orthopoxvirus Infection Inflammation/Immunology Cancer
    3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor [2]. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor . 3-Deazaneplanocin A hydrochloride also has anti-orthopoxvirus and anti-variola activities .
    3-Deazaneplanocin A hydrochloride
  • 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-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-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-13803R
    Tazemetostat (Standard)

    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-A0298
    EZH2-IN-2

    		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-16986
    EPZ011989
    3 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-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-131246
    DM-01

    		Histone Methyltransferase Cancer
    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 .
    DM-01
  • 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-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-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 [2].
    UNC2399
  • HY-161313
    DYB-03

    		Histone Methyltransferase HIF/HIF Prolyl-Hydroxylase Cancer
    DYB-03 is an oral active HIF-1α/EZH2 inhibitor. DYB-03 inhibits migration, invasion, and angiogenesis of lung cancer cells and HUVECs in vitro and in vivo. DYB-03 induces apoptosis in 2-ME2 - and GSK126 -resistant of A549 and H460 cells .
    DYB-03
  • 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-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-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-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-174372
    EZH2-IN-23

    		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-168131
    PROTAC EZH2 Degrader-3

    		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-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-12186G
    3-Deazaneplanocin A hydrochloride

    DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride

    		 Histone Methyltransferase Orthopoxvirus Infection Cancer
    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 [2].
    3-Deazaneplanocin A hydrochloride
  • 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-16986A
    EPZ011989 trifluoroacetate
    3 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-134899
    CPI-1328

    		Histone Methyltransferase Cancer
    CPI-1328 is an EZH2 inhibitor with a Ki value of 63 fM.
    CPI-1328
  • HY-156615
    Igermetostat

    		Histone Methyltransferase Cancer
    Igermetostat is EZH2 inhibitor, used in cancer research in vivo and in vitro .
    Igermetostat
  • HY-111085
    CPI-905

    		Histone Methyltransferase Cancer
    CPI-905 is a potent, selective, and cell-active EZH2 inhibitor .
    CPI-905
  • HY-13500R
    GSK343 (Standard)

    		Histone Methyltransferase Autophagy Cancer
    GSK343 (Standard) is the analytical standard of GSK343. This product is intended for research and analytical applications. GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.
    GSK343 (Standard)
  • HY-122115
    DCE_42

    		Histone Methyltransferase Cancer
    DCE_42 is a potent EZH2 inhibitor with an IC50 value of 22.6 µM. DCE_42 inhibits cell proliferation and has the potential for the research of lymphoma .
    DCE_42
  • HY-116605
    GSK926

    		Histone Methyltransferase Cancer
    GSK926 (compound 3) is a selective histone lysine methyltransferase EZH2 inhibitor (IC50=0.02 μM; Ki=7.9 nM), with SAM-competitive and cell-active properties. GSK926 can be used in cancer research .
    GSK926
  • 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-145762
    YM281

    		Apoptosis Histone Methyltransferase Cancer
    YM281 is a potent EZH2 inhibitor. YM281 induces cell apoptosis and cell cycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma .
    YM281
  • HY-116708
    DCE_254

    		Histone Methyltransferase Cancer
    DCE_254 is an EZH2 inhibitor (IC50=11 μM) that also exhibits significant antiproliferative activity against lymphoma cell lines. DCE_254 inhibits the development of hypermethylation-related cancers by inhibiting the SAM-mediated methyl transfer process (IC50=10.3 μM) .
    DCE_254
  • HY-169958
    EZH2-IN-22

    		Histone Methyltransferase Cancer
    EZH2-IN-22 (example 92) is a potent EZH2 inhibitor with IC50 values of <0.00051, <0.00051, 0.00052 µM for EZH2 (Y641N), EZH2 (Y641F), EZH2 (wt), respectively. EZH2-IN-22 shows antiproliferation activity .
    EZH2-IN-22
  • 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-117540
    ZLD10A

    		Histone Methyltransferase 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-169400
    HDACs/EZH2-IN-1

    		HDAC Histone Methyltransferase Apoptosis Cancer
    HDACs/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 .
    HDACs/EZH2-IN-1
  • HY-10442R
    3-Deazaneplanocin A (Standard)

    DZNep (Standard); 3-Deazaneplanocin (Standard)

    		 Reference Standards Histone Methyltransferase S-adenosylhomocysteine hydrolase (SAHH) Orthopoxvirus Infection Metabolic Disease Inflammation/Immunology Cancer
    3-Deazaneplanocin A (Standard) is the analytical standard of 3-Deazaneplanocin A (HY-10442). This product is intended for research and analytical applications. 3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor [2]. 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity .
    3-Deazaneplanocin A (Standard)
  • HY-182448
    TDI-11904

    		Histone Methyltransferase Cancer
    TDI-11904 is a peripherally active EZH2 inhibitor with an EZH2 IC50 of 0.9 nM. TDI-11904 inhibits EZH2 methyltransferase activity, reduces the trimethylation level of H3K27me3, and decreases intracellular H3K27me3 content. TDI-11904 inhibits the proliferation of lymphoma cells. TDI-11904 can be used for the research of lymphoma .
    TDI-11904

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