EN460

Name: EN460
Brand: MedChemExpress
SKU: HY-12837
Rating: 5.0 (9 reviews)

Cat. No.: HY-12837 Purity: 99.73%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

EN460 Chemical Structure

CAS No. : 496807-64-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 132	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 132	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 620	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

or Bulk Inquiry

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 9 publication(s) in Google Scholar

8 Publications Citing Use of MCE EN460

RT-PCR

: 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.

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Biological Activity
Purity & Documentation
References
Customer Review

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.

Molecular Weight

460.79

Formula

C₂₂H₁₂ClF₃N₂O₄

CAS No.

496807-64-8

Appearance

Solid

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

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.73%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (259 KB) HNMR (177 KB) LCMS (263 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

EN460 Related Classifications

Others

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EN460496807-64-8EN 460EN-460OthersInhibitorinhibitorinhibit

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EN460

Customer Review

EN460 Related Antibodies

8 Publications Citing Use of MCE EN460

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Complete Stock Solution Preparation Table

EN460 Related Classifications

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