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GSK 343 (CAS 1346704-33-3) is a potent, selective EZH2 inhibitor developed by GlaxoSmithKline. It targets EZH2, a histone methyltransferase within the Polycomb Repressive Complex 2 (PRC2), blocking its role in catalyzing H3K27me3, an epigenetic marker linked to gene silencing and cancer progression. With the molecular formula C₂₃H₂₅N₃O₃, it is used in oncology research to study epigenetic dysregulation in cancers (e.g., lymphoma, breast cancer) and explore therapeutic strategies. GSK 343 is cell-permeable, enabling in vitro and in vivo studies of tumor suppression and stem cell differentiation. Handle per lab safety protocols—research use only.
GSK 343 (CAS 1346704-33-3) is a potent, selective EZH2 inhibitor developed by GlaxoSmithKline. EZH2 (Enhancer of Zeste Homolog 2) is a histone methyltransferase within the Polycomb Repressive Complex 2 (PRC2), responsible for catalyzing H3K27me3 (trimethylation of histone H3 lysine 27), a marker of gene silencing.
Molecular Formula: C₂₃H₂₅N₃O₃.
Mechanism: Competitively inhibits EZH2, blocking aberrant H3K27 methylation linked to cancers (e.g., lymphoma, breast cancer).
Applications: Used in oncology research to study epigenetic regulation, tumor suppression, and therapeutic targeting.
Bioavailability: Cell-permeable, with in vitro and in vivo activity.
Explores EZH2's role in cancer progression and stem cell differentiation.
A tool compound for validating epigenetic drug targets.
Note: For research purposes only; handle per lab safety protocols.
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