MAK683

MAK683 (CAS No.: 1951408-58-4) is a class of synthetic small-molecule epigenetic modulators. As a selective inhibitor of embryonic ectoderm development protein EED (the reader and scaffold subunit of the polycomb repressive complex PRC2), it is derived from compound example 2 in patent US20160176882 A1 and is commonly referred to as EED inhibitor 1; by occupying the H3K27me3 recognition pocket of EED and exerting allosteric regulation, it inhibits the enzymatic activity of PRC2, reduces trimethylation of lysine 27 on histone H3, and induces remodeling of transcriptional programs associated with PRC2-regulated loci in cellular models. Based on various in vitro biochemical and biophysical evaluations (such as EED AlphaScreen binding, LC?MS and ELISA, and H3K27me3 peptide competition formats), MAK683 typically exhibits low-nanomolar inhibitory activity; at the cellular level, it likewise shows low-nanomolar effects, as reflected in study characterizations such as global H3K27me3 downregulation and proliferation inhibition in PRC2-dependent lymphoma cell systems. As a research tool compound, MAK683 is commonly used to elucidate EED-mediated signaling and epigenetic dependencies, validate target engagement through biomarkers such as H3K27me3 levels and gene expression changes, and support high-throughput or high-content screening and mechanism studies in human- or mouse-derived cell lines; the concentrations or doses used in experiments generally depend on the specific experimental design and research objectives. For research use only, not for human or veterinary use, and not for any form of ingestion or healthcare-related application.