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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related PRC2/EED Products |
|---|
| EEDi-5285
Eedi-5285 is a highly effective and orally active inhibitor of embryonic ectodermal development (EED). The IC50 value of BINDING EED protein is 0.2 nM, and it has anticancer activity. |
| EEDi-5273
Eedi-5273 is a potent and orally effective EED inhibitor (IC50 = 0.2 nM) that can achieve complete and sustained tumor regression. |
| 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. |
| FTX-6058
FTX-6058 is a potent, orally active embryonic ectodermal development (EED) inhibitor. FTX-6058 can induce HbF protein expression in both cell and murine models. FTX-6058 can be used in the study of specific hemoglobinopathies, including sickle cell disease and β-thalassemia. |
| 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. |
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