EN460
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货号：A312147
EN460是一种小分子抑制剂，能够抑制内质网氧化 1（ERO1），并选择性地与其还原活性形式（IC50 = 1.9 μM）相互作用，阻止其再氧化。
EN460 化学结构
EN460 3D分子结构
规格
价格
会员价
库存
数量
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EN460 纯度/质量文件 产品仅供科研
货号：A312147
标准纯度：
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产品说明书
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EN460 质控信息
EN460 生物活性
描述
EN460 is a small molecule inhibitor of endoplasmic reticulum oxidation 1 (ERO1) and interacts selectively (IC50=1.9 μM) with the reduced, active form of ERO1α and prevents its reoxidation.
EN460 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HeLa cells
20 μM
2 hours
Evaluate the inhibitory effect of EN460 and its analogs on VEGF secretion, results showed that I2 and I3 effectively inhibited VEGF secretion
Cell Death Dis. 2025 Feb 17;16(1):105
MM1.S cells
IC50 = 14.74 μM
72 hours
Inhibited cell proliferation
Bioorg Med Chem. 2019 Apr 15;27(8):1479-1488
U266 cells
25 μM
18 hours
Induced apoptosis
Bioorg Med Chem. 2019 Apr 15;27(8):1479-1488
ventricular myocytes (VMs)
20 µmol/L
5 minutes
EN460 inhibited Ero1α activity, reduced SR oxidation in TAB VMs, and improved Ca2+ handling
Circ Res. 2022 Mar 4;130(5):711-724
SJSA
8 μM
24 hours
Inhibiting ERO1 activity, reducing ROS production, thereby alleviating CYT997-induced apoptosis
J Exp Clin Cancer Res. 2019 Jan 31;38(1):44
143B
8 μM
24 hours
Inhibiting ERO1 activity, reducing ROS production, thereby alleviating CYT997-induced apoptosis
J Exp Clin Cancer Res. 2019 Jan 31;38(1):44
MiaPaca-2 cells
5 μM, 10 μM, 25 μM
24 hours
Inhibited migration and invasion of PDAC cells
J Immunol Res. 2021 Feb 23;2021:5553425
Capan-2 cells
5 μM, 10 μM, 25 μM
24 hours
Inhibited migration and invasion of PDAC cells
J Immunol Res. 2021 Feb 23;2021:5553425
Vero E6 cells
5 μM
36 hours
Inhibition of ERO1α activity, reducing PEDV-induced ROS generation and significantly suppressing PEDV replication
Vet Res. 2023 Feb 3;54(1):9
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EN460 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Rats
Hypertrophy induced by thoracic aortic banding (TAB)
Ex vivo heart perfusion
10 µmol/L
30 minutes
EN460 pretreatment significantly reduced the incidence of isoproterenol-induced ventricular fibrillation (VF) in TAB hearts, improving arrhythmia propensity
Circ Res. 2022 Mar 4;130(5):711-724
SCID mice
MDAMB231 tumor model
Intraperitoneal injection
10 mg/kg
Once daily for 6 days
Evaluate the effect of EN460 and I2 on tumor growth, results showed that EN460 and I2 slightly inhibited tumor growth and reduced VEGFA levels
Cell Death Dis. 2025 Feb 17;16(1):105
Zebrafish embryos
Zebrafish embryo model
E3 media
1-20 μM
6-30hpf
EN460 at a dose of 10 μM was significantly lethal during early embryonic development.
Bioorg Med Chem Lett. 2017 May 1;27(9):2029-2037
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EN460 参考文献
EN460 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.17mL
0.43mL
0.22mL
10.85mL
2.17mL
1.09mL
21.70mL
4.34mL
2.17mL
EN460 技术信息
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