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Apexbio Technology LLC GSK343 1346704-33-3 10mM (in 1mL DMSO)
Supplier: Apexbio Technology LLC A34495.1
GSK343 (CAS 1346704-33-3) is a selective SAM-competitive inhibitor targeting the histone lysine methyltransferase EZH2 which is the catalytic component of polycomb repressive complex 2 (PRC2) responsible for trimethylation of histone H3 at lysine 27 (H3K27me3) By competitively inhibiting EZH2 s methyltransferase activity GSK343 disrupts H3K27me3-mediated transcriptional silencing It shows potent inhibitory activity against EZH2 (IC50 4 nM) moderate inhibition against EZH1 (240 nM) but minimal impact on other SAM-dependent enzymes In vitro studies with various cancer cell models confirm its ability to reduce H3K27 trimethylation limit proliferation induce apoptosis promote autophagy and enhance chemosensitivity highlighting its utility as a research tool to study EZH2-related mechanisms
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