ERAP1-IN-1
Based on 5 publication(s) in Google Scholar
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.
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- 純度: 98.77%
- CAS 番号: 865273-97-8
- 分子式: C20H21F3N2O5S
- 分子量:458.45
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
生物活性
ERAP1[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
1 μM
Compound: 3
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Inhibition of ERAP1 in human HeLa cells stably expressing H-2 Kb infected with vaccinia virus containing ss-LEQLE-SIINFEKL epitope assessed as suppression of ss-LEQLE-SIINFEKL binding to MHC1 H-2 Kb at cell surface by measuring reduction in 25D1 staining
Inhibition of ERAP1 in human HeLa cells stably expressing H-2 Kb infected with vaccinia virus containing ss-LEQLE-SIINFEKL epitope assessed as suppression of ss-LEQLE-SIINFEKL binding to MHC1 H-2 Kb at cell surface by measuring reduction in 25D1 staining
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[PMID: 31841350] |
ERAP1-IN-1 (compound 3) allosterically activates ERAP1’s hydrolysis of fluorogenic and chromogenic amino acid substratesv[1].
ERAP1-IN-1 (50 μM) exhibits specific inhibition of ERAP1 in the cellular context[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 865273-97-8
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性状 Solid
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分子量 458.45
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分子式 C20H21F3N2O5S
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Color White to off-white
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SMILES
O=C(O)C1=CC=C(OC)C(S(=O)(NC2=CC(C(F)(F)F)=CC=C2N3CCCCC3)=O)=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Nature
2025 May;641(8061):202-210. PMID: 40140567 -
Proc Natl Acad Sci U S A
Controlling intracellular processing to enhance spherical nucleic acid immune stimulation. [Abstract]2025 Nov 11;122(45):e2409554122. PMID: 41183209 -
Front Microbiol
Endoplasmic Reticulum Aminopeptidase 1 Is Involved in Anti-viral Immune Response of Hepatitis B Virus by Trimming Hepatitis B Core Antigen to Generate 9-Mers Peptides. [Abstract]2022 May 4;13:829241. PMID: 35602060 -
bioRxiv
2025 Nov 30:2025.11.26.690562. PMID: 41394586 -
溶剤 & 溶解度
DMSO : 250 mg/mL (545.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1813 mL | 10.9063 mL | 21.8126 mL | 54.5316 mL |
| 5 mM | 0.4363 mL | 2.1813 mL | 4.3625 mL | 10.9063 mL | |
| 10 mM | 0.2181 mL | 1.0906 mL | 2.1813 mL | 5.4532 mL | |
| 15 mM | 0.1454 mL | 0.7271 mL | 1.4542 mL | 3.6354 mL | |
| 20 mM | 0.1091 mL | 0.5453 mL | 1.0906 mL | 2.7266 mL | |
| 25 mM | 0.0873 mL | 0.4363 mL | 0.8725 mL | 2.1813 mL | |
| 30 mM | 0.0727 mL | 0.3635 mL | 0.7271 mL | 1.8177 mL | |
| 40 mM | 0.0545 mL | 0.2727 mL | 0.5453 mL | 1.3633 mL | |
| 50 mM | 0.0436 mL | 0.2181 mL | 0.4363 mL | 1.0906 mL | |
| 60 mM | 0.0364 mL | 0.1818 mL | 0.3635 mL | 0.9089 mL | |
| 80 mM | 0.0273 mL | 0.1363 mL | 0.2727 mL | 0.6816 mL | |
| 100 mM | 0.0218 mL | 0.1091 mL | 0.2181 mL | 0.5453 mL |