Cat. No.: HY-133125

ERAP1-IN-1

5 Cited Publications

Customer Review

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.

For research use only. We do not sell to patients.

Purity: 98.77%
CAS No.: 865273-97-8
Formula: C₂₀H₂₁F₃N₂O₅S
Molecular Weight:458.45

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

ERAP1-IN-1 Chemical Structure

CAS No.: 865273-97-8

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (5)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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].

IC₅₀ & Target

ERAP1^[1]

All Aminopeptidase Isoforms :

CD13
LTA4H

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	1 μM Compound: 3	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	[PMID: 31841350]

In Vitro

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.

Chemical Information

CAS No. 865273-97-8
Appearance Solid
Molecular Weight 458.45
Formula C₂₀H₂₁F₃N₂O₅S
Color White to off-white
SMILES

O=C(O)C1=CC=C(OC)C(S(=O)(NC2=CC(C(F)(F)F)=CC=C2N3CCCCC3)=O)=C1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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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Nature

STING agonist-based ER-targeting molecules boost antigen cross-presentation. [Abstract]

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

Cancers modulate p53 truncal neoantigen display to evade T cell detection. [Abstract]

2025 Nov 30:2025.11.26.690562. PMID: 41394586
bioRxiv

January 30, 2022.

Solvent & Solubility

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1813 mL

10.9063 mL

21.8126 mL

5 mM

0.4363 mL

2.1813 mL

4.3625 mL

10 mM

0.2181 mL

1.0906 mL

2.1813 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Maben Z, et al. Discovery of Selective Inhibitors of Endoplasmic Reticulum Aminopeptidase 1. J Med Chem. 2019 Dec 30. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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ERAP1-IN-1

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) ERAP1-IN-1

All Aminopeptidase Isoforms

Biological Activity

Chemical Information

Publications (5)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

ERAP1-IN-1

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) ERAP1-IN-1

All Aminopeptidase Isoforms

Biological Activity

Chemical Information

Publications (5)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

ERAP1-IN-1 Related Classifications

HY-133125 Related Classifications