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PRC2

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48

Inhibitors & Agonists

1

Biochemical Assay Reagents

4

Peptides

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-101117
    EED226
    10+ Cited Publications

    Histone Methyltransferase Cancer
    EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model . EED226 is a potent, selective, and orally bioavailable EED inhibitor [2]. EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays .
    EED226
  • HY-158102
    Rinzimetostat
    1 Publications Verification

    ORIC-944

    Histone Methyltransferase Cancer
    Rinzimetostat (ORIC-944) is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). Rinzimetostat is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer.
    Rinzimetostat
  • HY-130708
    UNC6852
    4 Publications Verification

    Histone Methyltransferase PROTACs Cancer
    UNC6852 is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a von Hippel-Lindau ligand, with an IC50 of 247 nM for EED .
    UNC6852
  • 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-101512
    A-395
    4 Publications Verification

    Histone Methyltransferase Cancer
    A-395, a chemical probe, 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-132922

    APG-5918

    Histone Methyltransferase Cancer
    EEDi-5273 (APG-5918) is a potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 of 0.2 nM. EEDi-5273 can inhibit the polycomb repressive complex 2 (PRC2) activity and block trimethylation of histone H3 lysine 27. EEDi-5273 can be used for the research of cancer, such as ovarian cancer .
    EEDi-5273
  • HY-15647
    BRD9539
    1 Publications Verification

    Histone Methyltransferase Cancer
    BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1 .
    BRD9539
  • 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-130615
    PROTAC EED degrader-2
    1 Publications Verification

    PROTACs Histone Methyltransferase Cancer
    PROTAC EED degrader-2 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.11) targeting the EED subunit .
    PROTAC EED degrader-2
  • 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-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-130979

    Ligands for Target Protein for PROTAC Cancer
    EED226-COOH is an EED226-derived ligand for target protein EED ligand for PROTAC, binds to a ligand for VHL via linker to form UNC6852 (HY-130708) to degrade PRC2 .
    EED226-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-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-130614

    PROTACs Histone Methyltransferase Cancer
    PROTAC EED degrader-1 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit .
    PROTAC EED degrader-1
  • 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-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-152038

    Histone Methyltransferase Others
    SPEN-IN-1 (compound X1) is an inhibitor of SPEN which is a protein factor with a Kd value of 47 nM. SPEN-IN-1 has high selectivity for RepA, a 431-nucleotide domain in Xist (a non-coding RNA prototype) that comprises 8.5 units of a GC-rich motif responsible for gene silencing .
    SPEN-IN-1
  • HY-P2254

    Histone Methyltransferase Cancer
    H3K27(Me3) (15-34), a histone peptide, is a repressive chromatin mark derived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) [2].
    H3K27(Me3) (15-34)
  • HY-W003282

    Biochemical Assay Reagents Drug Intermediate Cancer
    3,6-Dibromo-2-methylpyridine is a key intermediate in organic synthesis. 3,6-Dibromo-2-methylpyridine can be used in the study of pulmonary fibrosis and PRC2-dependent cancers [2].
    3,6-Dibromo-2-methylpyridine
  • HY-158102A
    Rinzimetostat TFA
    1 Publications Verification

    ORIC-944 TFA

    Histone Methyltransferase Cancer
    Rinzimetostat (ORIC-944) TFA is the TFA salt form of ORIC (HY-158102). Rinzimetostat TFA is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). Rinzimetostat TFA is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer [2].
    Rinzimetostat TFA
  • HY-162384

    Histone Methyltransferase Cancer
    EPIC-0628 is an inhibitor of the HOTAIR-EZH2 interaction and promotes ATF3 expression. The long noncoding RNA HOTAIR has been found to regulate glioblastoma (GBM) progression and mediate DNA damage repair (DDR) by interacting with the catalytic subunit EZH2 of PRC2. EPIC-0628 also inhibits the ATF3-p38-E2F1 DDR pathway to inhibit the HR pathway and upregulates CDKN1A (p21) expression, causing cell cycle arrest. EPIC-0628 also synergizes with Temozolomide (TMZ) (HY-17364) to enhance its in vivo potency .
    EPIC-0628
  • 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
  • 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-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-132970

    Histone Methyltransferase Cancer
    EED ligand 1 is a diverse, potent, and efficacious inhibitor that target the EED subunit of the polycomb repressive complex 2 (PRC2) methyltransferase.
    EED ligand 1
  • HY-122640

    Histone Methyltransferase Cancer
    NPD13668 is an EZH2-mediated gene silencing modulator. NPD13668 inhibits EZH2/PRC2 (polycomb repressive complex 2) activity. NPD13668 reactivates the expression of silenced H3K27me3 target genes together with depletion of the H3K27me3 modification. NPD13668 can be used for the study of prostate cancer and ovarian cancer .
    NPD13668
  • HY-101512D

    Histone Methyltransferase Cancer
    rel-A-395 hydrochloride is the relative configuration of A-395 (HY-101512) hydrochloride. 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 .
    rel-A-395 hydrochloride
  • HY-P2252

    Histone Methyltransferase Cancer
    H3K27(Me) (15-34), a histone peptide, is a repressive chromatin markderived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) [2].
    H3K27(Me) (15-34)
  • HY-P2253

    Histone Demethylase Cancer
    H3K27(Me2) (15-34), a histone peptide, is a repressive chromatin mark derived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) [2].
    H3K27(Me2) (15-34)
  • HY-174397

    Histone Methyltransferase Epigenetic Reader Domain Cancer
    EED-IN-3 is an orally active EED inhibitor. EED-IN-3 effectively inhibits PRC2 by binding to EED (IC50 = 0.62 μM for EED) and downregulates H3K27me3. EED-IN-3 can efficiently and selectively inhibit PC3 cells with the IC50 of 3.69 μΜ and could significantly suppress colony formation and migration. EED-IN-3 can be used for research on prostate cancer.
    EED-IN-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-101117R

    Histone Methyltransferase Reference Standards Cancer
    EED226 (Standard) is the analytical standard of EED226 (HY-101117). This product is intended for research and analytical applications. EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model . EED226 is a potent, selective, and orally bioavailable EED inhibitor [2]. EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays .
    EED226 (Standard)
  • HY-117947

    Histone Methyltransferase Cancer
    (R)-OR-S1 is an isomer of OR-S1. The dual ZH1/2 inhibitors OR-S1 and OR-S2 exhibit strong inhibitory activity against both EZH1 and EZH2. OR-S1 and OR-S2 are highly selective methyltransferase inhibitors against EZH1 and EZH2, and they have very similar molecular features. Therefore, we investigated the effect of OR-S1 on acute myeloid leukemia (AML). We found that OR-S1 was able to induce cell differentiation and apoptosis in AML cells. These findings encouraged us to investigate whether functional LT-HSCs could survive PRC2-targeted therapy with OR-S1 or OR-S1 combined with cytarabine. The results showed that OR-S1 did not cause significant myelosuppression, and BM cells treated with the combination therapy were able to undergo normal hematopoiesis even 4 months after treatment. Therefore, temporary inhibition of EZH1 and EZH2 is clinically tolerable, making this combination therapy suitable for AML patients. AML is generally believed to originate from myeloid progenitor cells that inherit a large number of biological properties.
    (R)-OR-S1
  • HY-100846R

    Histone Methyltransferase Reference Standards Cancer
    JQEZ5 (Standard) is the analytical standard of JQEZ5 (HY-100846). This product is intended for research and analytical applications. 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 (Standard)
  • HY-101512R

    Reference Standards Histone Methyltransferase Cancer
    A-395 (Standard) is the analytical standard of A-395 (HY-101512). This product is intended for research and analytical applications. A-395, a chemical probe, 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 (Standard)
  • 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-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-130637

    PROTAC Linkers Cancer
    Boc-NH-PEG1-Ph-O-CH2COOH is a PROTAC Linker which is used for the EED-targeted PROTAC .
    Boc-NH-PEG1-Ph-O-CH2COOH
  • HY-130638

    VH032-O-Ph-PEG1-NH-Boc

    E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-O-Ph-PEG1-NH-Boc (VH032-O-Ph-PEG1-NH-Boc) is a synthesized E3 ligase ligand-linker conjugate which is used for the EED-targeted PROTAC .
    (S,R,S)-AHPC-O-Ph-PEG1-NH-Boc
  • HY-124660A

    Endogenous Metabolite Others
    A-395N serves as a control probe for A-395, a highly potent and selective chemical probe targeting the polycomb protein EED, a key player in Polycomb repressive complex 2 (PRC2) responsible for transcriptional repression via histone H3K27 methylation. While A-395N bears structural similarities to A-395, it demonstrates no pharmacological activity in biochemical or cellular assays, making it an ideal control compound.
    A-395N
  • 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-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-181308

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-13 (compound 4) 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 (compound 1) is a 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

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