EN4

製品コードS9807 バッチS980701

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₅H₂₄N₂O₄

分子量

416.47

CAS No.

1197824-15-9

Solubility (25°C)*

体外

DMSO

83 mg/mL (199.29 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）

Clear solution	5% DMSO 1 95% Corn oil	0.51mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 10.2 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.15mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 83 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.

* <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	EN4, a covalent ligand that targets cysteine 171 (C171) of MYC, is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.
in vitro	EN4 directly targets MYC in cells, reduces MYC and MAX thermal stability, inhibits MYC transcriptional activity, downregulates multiple MYC transcriptional targets, and impairs tumorigenesis. EN4 treatment significantly impairs 231MFP breast cancer cell proliferation in a dose- and time-dependent manner. EN4 impairs the cell survival of MYC transformed mammary epithelial MCF10A cells, but not parental MCF10A cells that are not dependent on MYC.^[1]
in vivo	EN4 treatment initiated after establishment of a 231MFP breast tumor xenograft in immune-deficient mice also significantly attenuates tumor growth in vivo.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	231MFP, MDA-MB-231, HEK293T and MCF10A cells
	濃度	50 μM
	反応時間	24 h
	実験の流れ	231MFP cells are seeded into 6 cm dishes and cells are treated with DMSO vehicle or EN4 (50 μM) for 24 h. Cells are harvested by scraping and RNA is isolated using Qiagen RNeasy mini kit with Qiagen DNase max kit to remove any DNA contamination. mRNA is enriched for using Oligo dT beads from the KAPA mRNA Capture Kit.
動物実験	動物モデル	C.B17 SCID female mice (6-8 weeks old)
	投薬量	50 mg/kg
	投与方法	IP

参考

[1] Lydia Boike, et al. Cell Chem Biol. 2021 Jan 21;28(1):4-13.e17.

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：

Sequential activation of E2F via Rb degradation and c-Myc drives resistance to CDK4/6 inhibitors in breast cancer [ Cell Rep, 2023, 42(11):113198]	PubMed: 37865915

Sequential activation of E2F via Rb degradation and c-Myc drives resistance to CDK4/6 inhibitors in breast cancer [ Cell Rep, 2023, 42(11):113198]

PubMed: 37865915

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。