MAK-683 is a potent inhibitor of embryonic ectoderm development protein (EED) and allosteric inhibitor of polycomb repressive complex 2 (PRC2), with 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).
MedKoo Cat#: 206940
Name: MAK-683
CAS#: 1951408-58-4
Chemical Formula: C20H17FN6O
Exact Mass: 376.1448
Molecular Weight: 376.40
Elemental Analysis: C, 63.82; H, 4.55; F, 5.05; N, 22.33; O, 4.25
Solvent | mg/mL | mM | |
---|---|---|---|
Solubility | |||
DMSO | 26.5 | 70.40 |
The following data is based on the product molecular weight 376.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |