1. Metabolic Enzyme/Protease Apoptosis
  2. Glutathione Peroxidase Ferroptosis
  3. JKE-1674

JKE-1674 is an orally active glutathione peroxidase 4 (GPX4) inhibitor and an active metabolite of GPX4 inhibitor ML-210. JKE-1674, an analog of ML-210 in which the nitroisoxazole ring is replaced with an α-nitroketoxime. JKE-1674 can convert into a nitrile oxide JKE-1777. JKE-1674 kills LOX-IMVI cells in a manner that is equipotent to ML-210 and is completely rescued by ferroptosis inhibitors.

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

JKE-1674 Chemical Structure

JKE-1674 Chemical Structure

CAS No. : 2421119-60-8

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

JKE-1674 is an orally active glutathione peroxidase 4 (GPX4) inhibitor and an active metabolite of GPX4 inhibitor ML-210. JKE-1674, an analog of ML-210 in which the nitroisoxazole ring is replaced with an α-nitroketoxime. JKE-1674 can convert into a nitrile oxide JKE-1777. JKE-1674 kills LOX-IMVI cells in a manner that is equipotent to ML-210 and is completely rescued by ferroptosis inhibitors[1][2][3].

IC50 & Target

GPX4[1]

In Vitro

JKE-1674 exhibits activity indistinguishable from that of ML210 in cellular target engagement assays including yielding the same +434Da GPX4 adduct in cells. JKE-1674 kills LOX-IMVI cells in a manner that is equipotent to ML210 and is completely rescued by ferroptosis inhibitors. JKE-1674 forms a nitrile-oxide electrophile in cells. JKE-1674 dehydration yields a nitrile-oxide electrophile that binds GPX4. JKE-1674 exhibits far greater stability than chloroacetamide inhibitors[1].

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

In Vivo

JKE-1674 (50 mg/kg; p.o.) can be detected in the serum of mice dosed orally with the compound[1].

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

Animal Model: SCID mice[1]
Dosage: 50 mg/kg (Pharmacokinetic Analysis)
Administration: P.o.
Result: Could be detected in the serum of mice dosed orally with the compound.
Molecular Weight

451.30

Formula

C20H20Cl2N4O4

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N1CCN(C(C2=CC=C(Cl)C=C2)C3=CC=C(Cl)C=C3)CC1)/C(C[N+]([O-])=O)=N/O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (221.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : ≥ 50 mg/mL (110.79 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2158 mL 11.0791 mL 22.1582 mL
5 mM 0.4432 mL 2.2158 mL 4.4316 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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% EtOH    90% PEG400

    Solubility: 5 mg/mL (11.08 mM); Clear solution; Need ultrasonic

  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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)

g

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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
References

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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.2158 mL 11.0791 mL 22.1582 mL 55.3955 mL
5 mM 0.4432 mL 2.2158 mL 4.4316 mL 11.0791 mL
10 mM 0.2216 mL 1.1079 mL 2.2158 mL 5.5396 mL
15 mM 0.1477 mL 0.7386 mL 1.4772 mL 3.6930 mL
20 mM 0.1108 mL 0.5540 mL 1.1079 mL 2.7698 mL
25 mM 0.0886 mL 0.4432 mL 0.8863 mL 2.2158 mL
30 mM 0.0739 mL 0.3693 mL 0.7386 mL 1.8465 mL
40 mM 0.0554 mL 0.2770 mL 0.5540 mL 1.3849 mL
50 mM 0.0443 mL 0.2216 mL 0.4432 mL 1.1079 mL
60 mM 0.0369 mL 0.1847 mL 0.3693 mL 0.9233 mL
80 mM 0.0277 mL 0.1385 mL 0.2770 mL 0.6924 mL
100 mM 0.0222 mL 0.1108 mL 0.2216 mL 0.5540 mL
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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.

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Product Name:
JKE-1674
Cat. No.:
HY-138153
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