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Description: MAK-683 (extracted from patent US20160176882 A1, compound example 2) is a novel and potent inhibitor of embryonic ectoderm development protein (EED) and allosteric inhibitor of polycomb repressive complex 2 (PRC2) with IC50s of 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay. It has potential antineoplastic activity. Upon administration, MAK683 selectively binds to the domain of EED that interacts with trimethylated lysine 27 on histone 3 (H3K27me3), which leads to a conformational change in the EED H3K27me3-binding pocket and prevents the interaction of EED with the histone methyltransferase enhancer zeste homolog 2 (EZH2).
References:
1. Chan, Ho Man, et al. TRIAZOLOPYRIMIDINE COMPOUNDS AND USES THEREOF. US20160176882 A1.
2. Huang D, et al. Binding Modes of Small-Molecule Inhibitors to the EED Pocket of PRC2. Chemphyschem. 2020 Feb 4; 21(3):263-271.
Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.
All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.
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Delivery expected until 9/6/2024
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