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MAK-683 is a potent inhibitor of embryonic ectoderm development protein (EED) and allosteric inhibitor of polycomb repressive complex 2 (PRC2). 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).
| Molecular Weight | 376.39 |
| Formula | C20H17FN6O |
| CAS Number | 1951408-58-4 |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PRC2/EED Products |
|---|
| EED226
EED226 is an effective, selective and orally active Polycomb reactive complex 2 (PRC2) inhibitor. When h3k27me0 peptide is used as substrate, ic50=23.4 nm; With mononucleosome as substrate, ic50=53.5 nm. It is a first in class, effective, orally bioavailable inhibitor of embryonic ectodermal development (EED) with strong anticancer effect. |
| A-395
A-395 is A Polycomb inhibitory complex 2 (Polycomb repressive complex 2; PRC2), a protein-protein interaction antagonist, inhibits the trimer PRC2 complex (ezh2-EED -SUZ12) with an IC50 value of 18 nM. |
| ORIC-944
ORIC-944 is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). ORIC-944 is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer. |
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