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Chemical Structure| 496807-64-8 Chemical Structure| 496807-64-8

Structure of EN460
CAS No.: 496807-64-8

Chemical Structure| 496807-64-8

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

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Product Details of EN460

CAS No. :496807-64-8
Formula : C22H12ClF3N2O4
M.W : 460.79
SMILES Code : 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
MDL No. :MFCD02951227

Safety of EN460

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HeLa cells 20 μM 2 hours Evaluate the inhibitory effect of EN460 and its analogs on VEGF secretion, results showed that I2 and I3 effectively inhibited VEGF secretion Cell Death Dis. 2025 Feb 17;16(1):105
MM1.S cells IC50 = 14.74 μM 72 hours Inhibited cell proliferation Bioorg Med Chem. 2019 Apr 15;27(8):1479-1488
U266 cells 25 μM 18 hours Induced apoptosis Bioorg Med Chem. 2019 Apr 15;27(8):1479-1488
ventricular myocytes (VMs) 20 µmol/L 5 minutes EN460 inhibited Ero1α activity, reduced SR oxidation in TAB VMs, and improved Ca2+ handling Circ Res. 2022 Mar 4;130(5):711-724
SJSA 8 μM 24 hours Inhibiting ERO1 activity, reducing ROS production, thereby alleviating CYT997-induced apoptosis J Exp Clin Cancer Res. 2019 Jan 31;38(1):44
143B 8 μM 24 hours Inhibiting ERO1 activity, reducing ROS production, thereby alleviating CYT997-induced apoptosis J Exp Clin Cancer Res. 2019 Jan 31;38(1):44
MiaPaca-2 cells 5 μM, 10 μM, 25 μM 24 hours Inhibited migration and invasion of PDAC cells J Immunol Res. 2021 Feb 23;2021:5553425
Capan-2 cells 5 μM, 10 μM, 25 μM 24 hours Inhibited migration and invasion of PDAC cells J Immunol Res. 2021 Feb 23;2021:5553425
Vero E6 cells 5 μM 36 hours Inhibition of ERO1α activity, reducing PEDV-induced ROS generation and significantly suppressing PEDV replication Vet Res. 2023 Feb 3;54(1):9

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Hypertrophy induced by thoracic aortic banding (TAB) Ex vivo heart perfusion 10 µmol/L 30 minutes EN460 pretreatment significantly reduced the incidence of isoproterenol-induced ventricular fibrillation (VF) in TAB hearts, improving arrhythmia propensity Circ Res. 2022 Mar 4;130(5):711-724
SCID mice MDAMB231 tumor model Intraperitoneal injection 10 mg/kg Once daily for 6 days Evaluate the effect of EN460 and I2 on tumor growth, results showed that EN460 and I2 slightly inhibited tumor growth and reduced VEGFA levels Cell Death Dis. 2025 Feb 17;16(1):105
Zebrafish embryos Zebrafish embryo model E3 media 1-20 μM 6-30hpf EN460 at a dose of 10 μM was significantly lethal during early embryonic development. Bioorg Med Chem Lett. 2017 May 1;27(9):2029-2037

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.85mL

2.17mL

1.09mL

21.70mL

4.34mL

2.17mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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