产品说明书
ERAP1-IN-1
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同义名 : | - |
| CAS号 : | 865273-97-8 | |
| 货号 : | A1339042 | |
| 分子式 : | C20H21F3N2O5S | |
| 纯度 : | 99%+ | |
| 分子量 : | 458.451 | |
| MDL号 : | MFCD07309764 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 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 |
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| 动物实验配方： |
| 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]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.18mL 0.44mL 0.22mL |
10.91mL 2.18mL 1.09mL |
21.81mL 4.36mL 2.18mL |
| 参考文献 |
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