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EED226

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Chemical Structure| 2083627-02-3 同义名 : MAK683
CAS号 : 2083627-02-3
货号 : A256458
分子式 : C17H15N5O3S
纯度 : 99%+
分子量 : 369.398
MDL号 : MFCD30738018
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(324.85 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • bromodomain

    EED, Kd:82 nM

    PRC2, Kd:114 nM
描述 EED226 functions as an inhibitor of the PRC2, targeting the K27me3-pocket of the EED protein. It has demonstrated significant antitumor efficacy in a xenograft mouse model[1]. EED226 stands out as a highly potent, efficient, and selective inhibitor of both EZH2 and EZH1, having been tested against a wide spectrum of epigenetic and non-epigenetic targets. It effectively diminishes the global H3K27Me3 mark in cells and exhibits selective cytotoxicity in cells with a heterozygous Y641N mutation. The permeability of EED226 is moderate, with measurements in Caco-2 cells showing an A→B permeability of 3.0x10-6 cm/s, and an efflux ratio of 7.6[2]. In vitro enzymatic assays reveal that EED226 is an inhibitor of PRC2, with an IC50 of 23.4 nM when using the H3K27me0 peptide as a substrate. Additionally, when the assay is conducted with mononucleosomes as the substrate and the stimulatory H3K27me3 present at 1× Kact (1.0 μM), EED226 exhibits an IC50 of 53.5 nM[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.54mL

2.71mL

1.35mL

27.07mL

5.41mL

2.71mL
参考文献

[1]Li L, et al. Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED. PLoS One. 2017 Jan 10;12(1):e0169855.

[2]Huang Y, et al. Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy. J Med Chem. 2017 Mar 23;60(6):2215-2226.

[3]Qi W, et al. An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED. Nat Chem Biol. 2017 Apr;13(4):381-388.