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EZH2 degrader

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Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-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-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-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-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-162250

    PROTACs Histone Methyltransferase Cancer
    MS8847 is a PROTAC degrader and antiproliferative agent targeting EZH2 (DC50=34.4 nM in EOL-1 MLL-rAML cells). MS8847 recruits the E3 ligase von Hippel-Lindau (VHL) to mediate the degradation of EZH2 via the ubiquitin-proteasome system. MS8847 induces antiproliferative effects in MLL-rearranged acute myeloid leukemia cells and inhibits the growth of triple-negative breast cancer cell lines or 3D triple-negative breast cancer models. MS8847 is applicable to research related to MLL-rearranged acute myeloid leukemia and triple-negative breast cancer .
    MS8847
  • HY-119198

    Apoptosis Histone Methyltransferase Cancer
    NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers .
    NSC745885
  • 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-157844

    PROTACs Histone Methyltransferase Cancer
    NUCC-0226272 is a potent PROTAC that targets EZH2 for degradation. NUCC-0226272 has anti-proliferative effect. NUCC-0226272 has the potential for cancer research .
    NUCC-0226272
  • HY-W014099

    PROTAC Linkers Cancer
    Boc-NH-C4-acid is a PROTAC linker, which belongs to a Alkyl/ether linker. Boc-NH-C4-acid can be used in the synthesis of the compound PROTAC1, and specifically degrades EED, EZH2, and SUZ12 in the PRC2 Complex.
    Boc-NH-C4-acid
  • 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-158239

    PROTACs E1/E2/E3 Enzyme Cancer
    MS181 (compound 1) is a potent cereblon (CRBN)-recruiting and EED-binding polycomb repressive complex 1 (PRC1) PROTAC degrader. MS181 decreases the expression of EED, EZH2, SUZ12, BMI1 and RING1B. MS181 shows antiproliferative activity (Strtucture Note: Red, EED binder (HY-158771); Blue, CRBN ligand (HY-41547); Black, Linker HY-131717) .
    MS181
  • HY-181326

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-25 (compound 10) is an EZH2-targeting PROTAC degrader. PROTAC EZH2 Degrader-25 triggers ubiquitination and subsequent proteasomal degradation of EZH2. PROTAC EZH2 Degrader-25 can be used for the research of lymphoma .
    PROTAC EZH2 Degrader-25
  • HY-181411

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-42 (compound 57) is an EZH2-targeting PROTAC degrader and antiproliferative agent. PROTAC EZH2 Degrader-42 induces cIAP-mediated ubiquitination and subsequent proteasomal degradation of EZH2. PROTAC EZH2 Degrader-42 can be used for the research of lymphoma .
    PROTAC EZH2 Degrader-42
  • HY-181308

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-13 is an EZH2-targeting PROTAC with an IC50 of 2.70 nM. PROTAC EZH2 Degrader-13 exerts antiproliferative effects in cancer cells. PROTAC EZH2 Degrader-13 can be used for the research of cancer .
    PROTAC EZH2 Degrader-13
  • HY-181323

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-22 (compound 7) is a PROTAC protein degrader targeting EZH2. PROTAC EZH2 Degrader-22 is applicable to cancer-related research .
    PROTAC EZH2 Degrader-22
  • HY-181305

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-10 is a selective PROTAC protein degrader targeting EZH2. PROTAC EZH2 Degrader-10 can be used for the research of cancer .
    PROTAC EZH2 Degrader-10
  • HY-181391

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-34 (compound E7 (13)) is an EZH2-target PROTAC degrader with a human EZH2 IC50 of 6.30 μM. PROTAC EZH2 Degrader-34 can be used for the research of pfeiffer cancer, prostate cancer .
    PROTAC EZH2 Degrader-34
  • 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-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
  • HY-181410

    PROTACs Histone Methyltransferase IAP Cancer
    PROTAC EZH2 Degrader-41 is an EZH2-targeting PROTAC and cIAP E3 ubiquitin ligase recruiter. PROTAC EZH2 Degrader-41 induces EZH2 degradation via ubiquitination and proteasomal breakdown. PROTAC EZH2 Degrader-41 exerts antiproliferative effects in lymphoma cells. PROTAC EZH2 Degrader-41 can be used for the research of lymphoma .
    PROTAC EZH2 Degrader-41
  • 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-181319

    PROTACs Histone Methyltransferase IAP Cancer
    PROTAC EZH2 Degrader-21 is an EZH2 degrader developed based on PROTAC technology. PROTAC EZH2 Degrader-21 induces the degradation of the target protein EZH2 via specific recruitment of the cIAP E3 ligase. PROTAC EZH2 Degrader-21 exhibits significant inhibitory activity in a variety of lymphoma cell lines. PROTAC EZH2 Degrader-21 can be used for research on the pathogenesis of lymphoma .
    PROTAC EZH2 Degrader-21
  • 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-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-181306

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-11 (compound 2) is a EZH2-targeting PROTAC protein degrader. PROTAC EZH2 Degrader-11 reduces tumor size and viability in 3D spheroid models. PROTAC EZH2 Degrader-11 can be used for the research of cancer .
    PROTAC EZH2 Degrader-11
  • HY-181320

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-19 (compound 6) is a is a PROTAC protein degrader targeting EZH2 with an IC50 of 15.00 nM. PROTAC EZH2 Degrader-19 induces strong degradation of all PRC2 subunits (EZH2, SUZ12, EED, RbAp48) in a concentration- and time-dependent manner.PROTAC EZH2 Degrader-19 exhibits antiproliferative effects in cancer cells.PROTAC EZH2 Degrader-19 can be used for the research of cancer .
    PROTAC EZH2 Degrader-19
  • 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-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-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-181392

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-35 (compound U3i (44)) is a PROTAC protein degrader targeting EZH2 with a human EZH2 Ka of 16.19 nM. PROTAC EZH2 Degrader-35 exhibits antiproliferative activity in triple-negative breast cancer cells and minimal cytotoxicity in normal human epithelial, hepatic, renal cells.PROTAC EZH2 Degrader-35 can be used for the research of triple-negative breast cancer .
    PROTAC EZH2 Degrader-35
  • HY-181300

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-17 (compound 52) is a PROTAC protein degrader targeting EZH2 with an antiproliferative IC50 of 18.32 μM in lymphoma cells. PROTAC EZH2 Degrader-17 exhibits antiproliferative activity against lymphoma cells. PROTAC EZH2 Degrader-17 can be used for the research of lymphoma .
    PROTAC EZH2 Degrader-17
  • HY-181354

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-36 (compound 15) is a PROTAC protein degrader targeting EZH2 with a target IC50 of 16.00 nM.PROTAC EZH2 Degrader-36 applicable to lymphoma-related research .
    PROTAC EZH2 Degrader-36
  • HY-181307

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-12 (compound 3) is a CRBN-recruiting PROTAC-based EZH2 degrader with an EZH2 IC50 of 3.90 nM and EZH1 IC50 of 5.24 μM .
    PROTAC EZH2 Degrader-12
  • HY-181318

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-20 (compound 54) is an EZH2-target PROTAC degrader with antiproliferative activity and IC50 values of about 10 μM against lymphoma cells. PROTAC EZH2 Degrader-20 can be used for the research of lymphoma .
    PROTAC EZH2 Degrader-20
  • HY-181301

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-18 (compound E-CH2-B4) is a PROTAC protein degrader targeting EZH2. PROTAC EZH2 Degrader-18 is applicable to lymphoma-related research .
    PROTAC EZH2 Degrader-18
  • HY-179499

    PROTACs Histone Methyltransferase Apoptosis Cancer
    PROTAC 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 .
    PROTAC EZH2 Degrader-9
  • HY-181412

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-43 (compound 59) is a PROTAC protein degrader targeting EZH2 with an IC50 of 21.73 μM against SU-DHL-6 cells. PROTAC EZH2 Degrader-43 can be used for the research of lymphoma .
    PROTAC EZH2 Degrader-43
  • HY-181355

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-28 (compound 66) is a PROTAC protein degrader targeting EZH2 with an IC50 of 16.2 μM against diffuse large B-cell lymphoma cells. PROTAC EZH2 Degrader-28 can be used for the research of lymphoma .
    PROTAC EZH2 Degrader-28
  • HY-181296

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-16 (compound 51) is a PROTAC protein degrader targeting EZH2 with an IC50 of 13.74 μM in SU-DHL-6 cells. PROTAC EZH2 Degrader-16 exerts antiproliferative activity against diffuse large B-cell lymphoma cells. PROTAC EZH2 Degrader-16 can be used for the research of diffuse large B-cell lymphoma .
    PROTAC EZH2 Degrader-16
  • HY-181414

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-45 (compound 61) is a PROTAC protein degrader targeting EZH2 with an IC50 of 22.97 μM in SU-DHL-6 cells. PROTAC EZH2 Degrader-45 can be used for the research of diffuse large b-cell lymphoma .
    PROTAC EZH2 Degrader-45
  • HY-181409

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-40 (compound 56) is a PROTAC protein degrader targeting EZH2 with an IC50 of 15.35 μM against SU-DHL-6 cells. PROTAC EZH2 Degrader-40 can be used for the research of diffuse large B-cell lymphoma .
    PROTAC EZH2 Degrader-40
  • HY-181359

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-30 (compound 67) is ais a PROTAC protein degrader targeting EZH2 with an IC50 of 6.22 μM against SU-DHL-6 cells. PROTAC EZH2 Degrader-30 can be used for the research of diffuse large B-cell lymphoma .
    PROTAC EZH2 Degrader-30
  • HY-181357

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-29 (compound 66) is a is a PROTAC protein degrader targeting EZH2 with an IC50 of 24.53 μM against diffuse large B-cell lymphoma cells. PROTAC EZH2 Degrader-29 can be used in studies related to diffuse large B-cell lymphoma .
    PROTAC EZH2 Degrader-29
  • HY-181360

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-31(compound 69) is a PROTAC protein degrader targeting EZH2, with antiproliferative IC50 values of 3.63 μM in lSU-DHL-6 cells and 8.74 μM in HBL-1 cells. PROTAC EZH2 Degrader-31 can be used for the research of lymphoma .
    PROTAC EZH2 Degrader-31
  • HY-181413

    PROTACs Histone Methyltransferase Bcl-2 Family Caspase PARP Cancer
    PROTAC EZH2 Degrader-44 (compound 60) is a highly efficient PROTAC degrader targeting the EZH2-PRC2 complex. By recruiting the CRBN E3 ligase and relying on the proteasome system, PROTAC EZH2 Degrader-44 simultaneously induces the degradation of core components EZH2, SUZ12 and EED, thereby significantly reducing the levels of H3K27me3 and CARM1. PROTAC EZH2 Degrader-44 exerts antiproliferative effects through a dual mechanism: on the one hand, it triggers mitochondrial dysfunction leading to decreased membrane potential; on the other hand, it strongly promotes apoptosis by regulating Bcl-2 family proteins (upregulating Bax, Caspase-3 and PARP, and downregulating Bcl-2). PROTAC EZH2 Degrader-44 exhibits only extremely low cytotoxicity in human normal mammary epithelial, liver and kidney cells, showing a favorable safety window. PROTAC EZH2 Degrader-44 is an ideal tool molecule for exploring the mechanisms of targeted therapy for triple-negative breast cancer .
    PROTAC EZH2 Degrader-44
  • HY-181295

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-14 is an EZH2 PROTAC degrader, with an IC50 of 18.21 μM against diffuse large B-cell lymphoma cells, and exhibits no antiproliferative activity against non-target cells at concentrations up to 30.00 μM. PROTAC EZH2 Degrader-14 can be used in studies related to diffuse large B-cell lymphoma .
    PROTAC EZH2 Degrader-14
  • HY-178694

    Histone Methyltransferase Cancer
    DC-PRC2in-01 is a potent EZH2-EED interaction inhibitor with an IC50 of 4.21 μM and a Kd of 4.56 μM. DC-PRC2in-01 disrupts the EZH2-EED interaction, leading to degradation of PRC2 core proteins and decrease of H3K27me3 levels, inhibition of PRC2-driven lymphoma cell proliferation, and cell cycle arrest. DC-PRC2in-01 can be used for the research of PRC2-related cancers, such as Diffuse Large B-cell Lymphoma (DLBCL) and follicular lymphoma (FL) .
    DC-PRC2in-01

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