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 . (Pink: EZH2 ligand ( HY-147230 ); Blue: VHL ligand ( HY-125845 ); Black: linker).
Products | Products > Disease Areas > Cancer | Products > Disease Areas > Breast Cancer | Products > Disease Areas > Triple-Negative Breast Cancer | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Epigenetics | Products > Signaling Pathways > Apoptosis | Products > Signaling Pathways > Cell Cycle/DNA Damage | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Signaling Pathways > PARP | Products > Signaling Pathways > PROTACs | Products > Signaling Pathways > Histone Methyltransferase | Products > Signaling Pathways > Bcl-2 Family | Products > Signaling Pathways > Caspase
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