2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase
  5. EZH2 Isoform
  6. EZH2 Degrader

EZH2 Degrader

EZH2 Degraders (9):

Cat. No. Product Name Effect Purity
  • HY-181333
    PROTAC EZH2 Degrader-38
    		Degrader
    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.
  • HY-141877
    MS4322
    		Degrader 99.14%
    MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )).
  • HY-157844
    NUCC-0226272
    		Degrader 99.68%
    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.
  • HY-157164
    PROTAC EZH2 Degrader-2
    		Degrader 98.77%
    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.
  • HY-147090
    Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH
    		Degrader 99.06%
    Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH (Compound 21b) incorporates a ligand for EZH2, and a PROTAC linker, which recruit E3 ligases. Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH (Compound 21b) can be used for the research of lymphoma.
  • HY-179499
    PROTAC EZH2 Degrader-9
    		Degrader
    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.
  • HY-181327
    PROTAC EZH2 Degrader-26
    		Degrader
    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.
  • HY-181413
    PROTAC EZH2 Degrader-44
    		Degrader
    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.
  • HY-181319
    PROTAC EZH2 Degrader-21
    		Degrader
    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.