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EN4 {[allProObj[0].p_purity_real_show]}

货号:A1060062

EN4是一种针对MYC的半胱氨酸171 (C171) 的共价配体,具有高选择性和抗肿瘤作用。它有效下调MYC靶标,在癌症研究中具有重要应用。

EN4 化学结构 CAS号:1197824-15-9
EN4 化学结构
CAS号:1197824-15-9
EN4 3D分子结构
CAS号:1197824-15-9
EN4 化学结构 CAS号:1197824-15-9
EN4 3D分子结构 CAS号:1197824-15-9
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EN4 纯度/质量文件 产品仅供科研

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EN4 生物活性

描述 EN4 is a covalent ligand designed to target cysteine 171 (C171) of MYC. It exhibits selectivity for c-MYC over N-MYC and L-MYC. Moreover, EN4 effectively inhibits MYC transcriptional activity.
体内研究

The administration of EN4 (50 mg/kg; intraperitoneal injection; daily; for 3 weeks) led to a significant reduction in tumor growth in 231MFP breast tumor xenograft mice[1].

体外研究

EN4 treatment at concentrations ranging from 1 to 50 μM for 72 hours markedly reduces proliferation of 231MFP breast cancer cells in a dose-dependent manner, achieving over 90% inhibition of proliferation at 50 μM[1].

EN4 treatment at a concentration of 50 μM for 60 hours significantly reduces the protein levels of representative MYC-regulated target genes, such as CDK2 and CDC25A. Additionally, EN4 treatment markedly decreases MYC levels[1].

EN4 demonstrates potent inhibition of both MYC/MAX binding to its DNA consensus sequence in vitro and MYC transcriptional activity in cells. It inhibits MYC/MAX binding to the E-box response element DNA consensus sequence in a dose-dependent manner, with an IC50 value of 6.7 μM. Additionally, EN4 inhibits MYC luciferase reporter activity in a dose-dependent manner, with an IC50 value of 2.8 μM[1].

EN4 treatment (50 μM; for 2 hours) resulted in a significant reduction in the thermal stability of MYC in 231MFP breast cancer cells[1].

EN4 参考文献

[1]Lydia Boike, et al. Discovery of a Functional Covalent Ligand Targeting an Intrinsically Disordered Cysteine within MYC. Cell Chem Biol. 2021 Jan 21;28(1):4-13.e17.

EN4 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

12.01mL

2.40mL

1.20mL

24.01mL

4.80mL

2.40mL

EN4 技术信息

CAS号1197824-15-9
分子式C25H24N2O4
分子量 416.469
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,Room Temperature

溶解度

DMSO: 120 mg/mL(288.14 mM),配合低频超声助溶,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

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