ERAP1-IN-1 | ERAP1 Inhibitor | AmBeed-信号通路专用抑制剂

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ERAP1-IN-1 {[allProObj[0].p_purity_real_show]}

货号：A1339042

ERAP1-IN-1 is an endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor. ERAP1-IN-1 competitively inhibits ERAP1 activity towards a nonamer peptide representative of physiological substrates[1].

ERAP1-IN-1 化学结构
CAS号：865273-97-8

ERAP1-IN-1 3D分子结构
CAS号：865273-97-8

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ERAP1-IN-1 纯度/质量文件产品仅供科研

货号：A1339042 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell Host Microbe, 2024. Ambeed. [ A163338 ]; • Cancer Res., 2024. Ambeed. [ A295334 ]; • J. Pharm. Investig., 2024. Ambeed. [ A221527 , A691302 , A272538 , A187261 ]; • J. Fungi, 2024, 10(11): 751. Ambeed. [ A796919 ]; • JBC, 2024, 107935. Ambeed. [ A194396 ]; 更多 >

ERAP1-IN-1 生物活性

描述

ERAP1 is an endoplasmic reticulum-resident zinc aminopeptidase that plays an important role in the immune system by trimming peptides for loading onto major histocompatibility complex proteins. ERAP1-IN-1 is an activator of ERAP1 L-AMC hydrolysis and also a very weak inhibitor of ERAP2 with an IC₅₀ greater than 200 μM. ERAP1-IN-1 activated ERAP1 hydrolysis of L-AMC with an AC₅₀ of 3.7 μM and a maximum activity enhancement of 4.1-fold over control. ERAP1-IN-1 inhibited peptide hydrolysis in a dose-dependent manner. Increasing concentrations of ERAP1-IN-1 resulted in increased rather than decreased L-pNA hydrolysis activity, across a range of substrate concentrations indicating that ERAP1-IN-1 is acting as a non-essential activator of L-pNA hydrolysis. ERAP1-IN-1 exhibited specific inhibition of ERAP1 in the cellular context with an IC₅₀ of 1 μM. ERAP1-IN-1 activated all three ERAP1 alleles but was a more potent activator of disease-associated allele II, which it activated with sub-micromolar AC₅₀^[2].

作用机制

For ERAP1-IN-1, the top in silico docking solutions outside the active site were found at the junction of domains II and IV^[2].

ERAP1-IN-1 参考文献

[1]Maben Z, Arya R, Rane D, et al. Discovery of Selective Inhibitors of Endoplasmic Reticulum Aminopeptidase 1. J Med Chem. 2020;63(1):103-121.

[2]Maben Z, et al. Discovery of Selective Inhibitors of Endoplasmic Reticulum Aminopeptidase 1. J Med Chem. 2020 Jan 9;63(1):103-121

ERAP1-IN-1 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.91mL

2.18mL

1.09mL

21.81mL

4.36mL

2.18mL

ERAP1-IN-1 技术信息

CAS号	865273-97-8
分子式	C₂₀H₂₁F₃N₂O₅S
分子量	458.451

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 250 mg/mL(545.31 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

动物实验配方

摩尔计算器

计算溶液所需的质量，体积或浓度。 Ambeed 摩尔浓度计算器基于以下方程式：

浓度 (mol/L) × 体积 (L) × 分子量 (g/mol)=质量 (g)

浓度

体积

分子量

质量

ERAP1-IN-1 {[allProObj[0].p_purity_real_show]}

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ERAP1-IN-1 {[allProObj[0].p_purity_real_show]}

ERAP1-IN-1 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

ERAP1-IN-1 质控信息

ERAP1-IN-1 生物活性

ERAP1-IN-1 参考文献

ERAP1-IN-1 实验方案

ERAP1-IN-1 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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ERAP1-IN-1 纯度/质量文件产品仅供科研