Cat. No.: HY-12837

EN460

15 Cited Publications

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Based on 15 publication(s) in Google Scholar

EN460 is a selective endoplasmic reticulum oxidation 1 (ERO1) inhibitor. EN460 (IC₅₀ of 1.9 μM) interacts selectively with the reduced, active form of ERO1α and prevents its reoxidation.

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Pureté: 99.94%
CAS No.: 496807-64-8
Formule: C₂₂H₁₂ClF₃N₂O₄
Masse moléculaire:460.79

Stockage:

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

EN460 Chemical Structure

CAS No.: 496807-64-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- Cellular Effect
- In Vitro
Chemical Information
Publications (15)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Cellular Effect

Cell Line	Type	Value	Description	References
MM1.S	IC₅₀	14.74 μM Compound: EN460	Cytotoxicity against human MM1S cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human MM1S cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 30850265]
U-266	IC₅₀	10.1 μM Compound: EN460	Cytotoxicity against human U266 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human U266 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 30850265]

In Vitro

Exposure of cells to EN460 or QM295 resulted in the accumulation of an ERO1α form with lower mobility, indicative of the reduced state. EN460 and QM295 were also found to activate an unfolded protein response reporter in cultured 293T cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 496807-64-8
Appearance Solid
Masse moléculaire 460.79
Formule C₂₂H₁₂ClF₃N₂O₄
Color Pink to red
SMILES

FC(F)(F)C1=NN(C2=CC(C(O)=O)=C(Cl)C=C2)C(/C1=C\C3=CC=C(C4=CC=CC=C4)O3)=O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (15)

All Cell Proliferation/Viability AssayWBCell Imaging/StainingFlow CytometryRT-PCR

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Journal Impact Factor

Nat Cell Biol

ERO1a fosters glioblastoma aggressiveness and metabolic flexibility by regulating mitochondria-associated membrane dynamics. [Abstract]

2026 Jun 12. PMID: 42286227
J Adv Res

LPCAT3 deficiency Drives phospholipid remodeling and mitochondrial oxidative dysfunction to accelerate MASH-HCC development. [Abstract]

2026 Apr 6:S2090-1232(26)00298-5. PMID: 41951050
J Exp Clin Cancer Res

CYT997(Lexibulin) induces apoptosis and autophagy through the activation of mutually reinforced ER stress and ROS in osteosarcoma. [Abstract]

2019 Jan 31;38(1):44. PMID: 30704503

EN460 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Jan 31;38(1):44. [Abstract]

143B cells are treated with CYT997 (80 nM) and/or EN460 (8 μM) for 24 h, and apoptosis, autophagy and ER stress-related proteins including c-PARP, caspase-4, LC3B, Beclin-1, CHOP and ERO1 are analyzed by western blotting.
J Exp Med

ASC deglutathionylation is a checkpoint for NLRP3 inflammasome activation. [Abstract]

2021 Sep 6;218(9):e20202637. PMID: 34342641
Diabetes Metab J

Serpina3c Mitigates Adipose Tissue Inflammation by Inhibiting the HIF1α-Mediated Endoplasmic Reticulum Overoxidation in Adipocytes. [Abstract]

2026 Jan;50(1):62-76. PMID: 40403760
Free Radic Biol Med

2026 Feb 16:244:452-463. PMID: 41422996
Ecotoxicol Environ Saf

Mitochondrial dysfunction and endoplasmic reticulum stress induced by activation of PPARα leaded testicular to apoptosis in SD rats explored to di-(2-ethylhexyl) phthalate (DEHP). [Abstract]

2023 Dec:268:115711. PMID: 37979351
Biomed J

IRE1-Mediated Endoplasmic Reticulum Stress Response Regulates Oxidative Damage in CYP4V2 Deficient Human Retinal Pigment Epithelial Cells. [Abstract]

2025 Aug;48(4):100875. PMID: 40466971

EN460 purchased from MedChemExpress. Usage Cited in: Biomed J. 2025 Aug;48(4):100875. [Abstract]

EN460 (5, 10, 15 μM), an ERO1-Lα inhibitor, regulated ERO1A mRNA.

EN460 purchased from MedChemExpress. Usage Cited in: Biomed J. 2025 Aug;48(4):100875. [Abstract]

H2DCFDA staining of intracellular ROS (EN460 15 μM, 48 h).
Int J Mol Sci

Hepatocyte-Derived Prostaglandin E2-Modulated Macrophage M1-Type Polarization via mTOR-NPC1 Axis-Regulated Cholesterol Transport from Lysosomes to the Endoplasmic Reticulum in Hepatitis B Virus x Protein-Related Nonalcoholic Steatohepatitis. [Abstract]

2022 Oct 1;23(19):11660. PMID: 36232960
Prog Neurobiol

ERO1A inhibition mitigates neuronal ER stress and ameliorates UBQLN2ALS phenotypes in Drosophila melanogaster. [Abstract]

2024 Nov:242:102674. PMID: 39395630
Fish Shellfish Immunol

Grass Carp Reovirus (GCRV) infection activates the PERK-eIF2α pathway to promote the viral replication. [Abstract]

2024 Dec:155:110020. PMID: 39528019
Vet Res

Regulatory effects of Trichinella spiralis serpin-type serine protease inhibitor on endoplasmic reticulum stress and oxidative stress in host intestinal epithelial cells. [Abstract]

2024 Jun 14;55(1):78. PMID: 38877574

EN460 purchased from MedChemExpress. Usage Cited in: Vet Res. 2024 Jun 14;55(1):78. [Abstract]

EN460 at dosages of 0, 4, 8, 12, 16, and 20 mM were cocultured with IPEC for 1 h, respectively. Then, a CCK-8 cell activity detection kit was used to determine the optimal interaction concentration.
Vet Res

Porcine epidemic diarrhea virus activates PERK-ROS axis to benefit its replication in Vero E6 cells. [Abstract]

2023 Feb 3;54(1):9. PMID: 36737830

EN460 purchased from MedChemExpress. Usage Cited in: Vet Res. 2023 Feb 3;54(1):9. [Abstract]

Vero E6 cells were infected with PEDV with or without EN460 (5 μM). Dimethylsulfoxide (DMSO) was used as solvent control. A The effects of ERO1α inhibition on CHOP, ERO1α, and PEDV N expression were shown by Western blotting with β-actin used as loading control.

EN460 purchased from MedChemExpress. Usage Cited in: Vet Res. 2023 Feb 3;54(1):9. [Abstract]

Vero E6 cells were infected with PEDV with or without EN460 (5 μM). Dimethylsulfoxide (DMSO) was used as solvent control. Cells collected at 36 hpi were measured for changes in cytosolic ROS level by flow cytometry after incubation with 10 μM DCFH-DA for 30 min at 37 °C.
Vet Microbiol

Porcine circovirus type 2 induces CHOP-ERO1α-ROS-mediated apoptosis in PK-15 cells. [Abstract]

2022 Oct:273:109548. PMID: 36037618
bioRxiv

2025 Oct 6.

Solvant et solubilité

In Vitro:

DMSO : 12.5 mg/mL (27.13 mM; ultrasonic and warming and heat to 60°C; 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

2.1702 mL

10.8509 mL

21.7019 mL

5 mM

0.4340 mL

2.1702 mL

4.3404 mL

10 mM

0.2170 mL

1.0851 mL

2.1702 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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: ≥ 1.67 mg/mL (3.62 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 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 (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.25 mg/mL (2.71 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 1.25 mg/mL (2.71 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 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)
Instruction de manipulation (2659 KB)

Références

[1]. Blais JD, et al. A small molecule inhibitor of endoplasmic reticulum oxidation 1 (ERO1) with selectively reversible thiol reactivity. J Biol Chem. 2010 Jul 2;285(27):20993-1003. [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	2.1702 mL	10.8509 mL	21.7019 mL	54.2546 mL
	5 mM	0.4340 mL	2.1702 mL	4.3404 mL	10.8509 mL
	10 mM	0.2170 mL	1.0851 mL	2.1702 mL	5.4255 mL
	15 mM	0.1447 mL	0.7234 mL	1.4468 mL	3.6170 mL
	20 mM	0.1085 mL	0.5425 mL	1.0851 mL	2.7127 mL
	25 mM	0.0868 mL	0.4340 mL	0.8681 mL	2.1702 mL

Keywords

EN460

15 Cited Publications

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EN460

Covalent Screening Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Covalent Screening Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Infection Compound Library

Publications Citing Use of MedChemExpress (MCE) EN460

Activité biologique

Chemical Information

Publications (15)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

EN460

Covalent Screening Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Covalent Screening Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Infection Compound Library

Publications Citing Use of MedChemExpress (MCE) EN460

Activité biologique

Chemical Information

Publications (15)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

EN460 Related Classifications

HY-12837 Related Classifications