MAK683

製品コードS8983 バッチS898301

印刷

化学情報

Synonyms

EED inhibitor-1

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₀H₁₇FN₆O

分子量

376.39

CAS No.

1951408-58-4

Solubility (25°C)*

体外

DMSO

12.5 mg/mL (33.21 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.300mg/ml (0.80mM)	Taking the 1 mL working solution as an example, add 50 μL of 6 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.150mg/ml (0.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	MAK683 (EED inhibitor-1, example 2) is an inhibitor of embryonic ectoderm development (EED). MAK683 exhibits IC50 of 59 nM, 89 nM and 26 nM in EED Alphascreen binding, LC-MS and ELISA assay, respectively.
in vitro	MAK-683 binds to EED and disrupts the PRC2 complex. Cell viability is not significantly affected and the levels of H3K27me3 are decreased. A significant increase in the percentage of mature PCs after this compound treatment in association with a higher CD38 expression is also identified.^[3]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MBCs
	濃度	2 µM
	反応時間	4 days, 3 days
	実験の流れ	MBCs are differentiated using a previously described culture protocol. All cultures are performed in Iscove modified Dulbecco medium, 10% FCS and 25–35% of Resto-6 cells supernatant. 1.5 × 10⁵/ml purified peripheral blood MBCs are activated for 4 days by 10 µg/ml of phosphorothioate CpG oligodeoxynucleotides (ODN) 2006, 50 ng/ml histidine tagged soluble CD40 ligand (CD40L) and 5 µg/ml of an anti-poly-histidine mAb in the presence of 20 U/ml IL-2, 50 ng/ml IL-10, and 10 ng/ml IL-15. The next 3 days, PBs are generated by removing ODN and CD40L and changing the cytokine cocktail. From day 7 to day 10, PBs are differentiated into early PCs by adding 50 ng/ml IL-6, 10 ng/ml IL-15, 500 U/ml IFN-α. This compound is added at the start of each step and its effects are evaluated by analyzing cell counts and phenotype at the end of each step.

参考

https://patents.google.com/patent/US20160176882A1/en
https://pubmed.ncbi.nlm.nih.gov/31816138/
https://pubmed.ncbi.nlm.nih.gov/30755708/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

EED Maintains the Small Cell Lung Cancer Neuroendocrine Phenotype and Drives Lung Cancer Histological Transformation [ bioRxiv, 2025, 2025.07.07.663486]	PubMed: 40672300
AKT and EZH2 inhibitors kill TNBCs by hijacking mechanisms of involution [ Nature, 2024, 10.1038/s41586-024-08031-6]	PubMed: 39385030
Activation of automethylated PRC2 by dimerization on chromatin [ Mol Cell, 2024, 84(20):3885-3898.e8]	PubMed: 39303719
PPARγ and C/EBPα enable adipocyte differentiation upon inhibition of histone methyltransferase PRC2 in malignant tumors [ J Biol Chem, 2024, 300(10):107765]	PubMed: 39276936
Combating castration-resistant prostate cancer by co-targeting the epigenetic regulators EZH2 and HDAC [ PLoS Biol, 2023, 21(4):e3002038]	PubMed: 37104245
Induction of senescence-associated secretory phenotype underlies the therapeutic efficacy of PRC2 inhibition in cancer [ Cell Death Dis, 2022, 13(2):155]	PubMed: 35169119
ARID1A-deficient bladder cancer is dependent on PI3K signaling and sensitive to EZH2 and PI3K inhibitors [ JCI Insight, 2022, e155899]	PubMed: 35852858

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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