JKE-1674
Based on 6 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.97%
- CAS. Nr.: 2421119-60-8
- Formel: C20H20Cl2N4O4
- Molecular Weight:451.30
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Immunology/Inflammation Compound Library
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HY-L034
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Oxygen Sensing Compound Library
HY-L045
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Ferroptosis Compound Library
HY-L051
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Orally Active Compound Library
HY-L061
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Anti-Cancer Metabolism Compound Library
HY-L083
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Targeted Diversity Library
HY-L099
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Publications Citing Use of MedChemExpress (MCE) JKE-1674
More- Cancer Discov. 2024 Aug 2;14(8):1476-1495. [Abstract]
- Redox Biol. 2024 Nov 5:78:103419. [Abstract]
- Adv Sci (Weinh). 2025 May 20:e01042. [Abstract]
- J Ethnopharmacol. 2026 Feb 28:357:120890. [Abstract]
- Front Biosci (Landmark Ed). 2025 Aug 30;30(8):42844. [Abstract]
- Breast Cancer Res Treat. 2024 Nov;208(2):307-320. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
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Flow Cytometry
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IHC
Biologische Aktivität
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GPX4 |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice[1]
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Dosage:50 mg/kg (Pharmacokinetic Analysis)
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Administration:P.o.
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Result:Could be detected in the serum of mice dosed orally with the compound.
Chemical Information
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CAS. Nr. 2421119-60-8
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Appearance Solid
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Molecular Weight 451.30
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Formel C20H20Cl2N4O4
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Color Off-white to light yellow
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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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (6)
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Journal Impact Factor
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Most Recent
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Cancer Discov
BRCA1-mediated dual regulation of ferroptosis exposes a vulnerability to GPX4 and PARP co-inhibition in BRCA1-deficient cancers. [Abstract]2024 Aug 2;14(8):1476-1495. PMID: 38552003
JKE-1674 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2024 Aug 2;14(8):1476-1495. [Abstract]
Cell death in Cas9 control or BRCA1-sgRNA-infected SKOV3 cells treated with 10μM olaparib (48 hours), 5μM niraparib (48 hours), and/or 5μM JKE-1674 (24 hours) in the absence or presence of ferrostatin-1.
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Redox Biol
Reactivation of MAPK-SOX2 pathway confers ferroptosis sensitivity in KRASG12C inhibitor resistant tumors. [Abstract]2024 Nov 5:78:103419. PMID: 39527862
JKE-1674 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Nov 5:78:103419. [Abstract]
Cell viability of the control NCI-H358, Calu-1 cells and the corresponding resistant cell lines of treatment with increasing concentrations of JKE-1674 for 24 h (NCI-H358-derived cells: 0.25-5 μM, Calu-1-derived cells: 0.0625-1 μM). JKE-1674 reduced the viability of AMG510- and MRTX849-resistant cells more markedly than that of the corresponding parental cells.
JKE-1674 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Nov 5:78:103419. [Abstract]
Representative phase-contrast images of the control NCI-H358, Calu-1 cells and their corresponding AMG510- and MRTX849-resistant cells after treatment with JKE-1674 (1 μM; 12 h).
JKE-1674 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Nov 5:78:103419. [Abstract]
MDA contents in the control NCI-H358, Calu-1 cells and their corresponding AMG510- and MRTX849-resistant cells after treatment with JKE-1674 (1 μM; 12 h). JKE-1674 increased MDA contents, with greater increases in the AMG510- and MRTX849-resistant cells than in the corresponding parental cells.
JKE-1674 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Nov 5:78:103419. [Abstract]
Flow cytometry analysis of oxidized BODIPY dye and quantification of median fluorescence intensity in the control NCI-H358, Calu-1 cells and their corresponding AMG510- and MRTX849-resistant cells after treatment with JKE-1674 (1 μM; 12 h).
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Adv Sci (Weinh)
Targeting GPX4 to Induce Ferroptosis Overcomes Chemoresistance Mediated by the PAX8-AS1/GPX4 Axis in Intrahepatic Cholangiocarcinoma. [Abstract]2025 May 20:e01042. PMID: 40391780
JKE-1674 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 May 20:e01042. [Abstract]
Ki-67 and 4-HNE immunohistochemical staining in patient-derived organoids after treatment with JKE-1674, alone or in combination with gemcitabine (5 μM), for 72 h. JKE-1674 combined with gemcitabine decreased Ki-67 levels and increased 4-HNE levels.
JKE-1674 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 May 20:e01042. [Abstract]
Images and weights of subcutaneous tumors from the P7 patient-derived organoid xenograft model after JKE-1674 (25 mg/kg; p.o.; three times weekly; 8 weeks), alone or in combination with gemcitabine and cisplatin. JKE-1674 significantly enhanced the tumor growth inhibition produced by the gemcitabine-cisplatin combination in the PDOX model.
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J Ethnopharmacol
Paris polyphylla Smith var. yunnanensis-derived saponins potentiate the antitumor activity of GPX4 inhibitors. [Abstract]2026 Feb 28:357:120890. PMID: 41232632 -
Front Biosci (Landmark Ed)
Immune Characteristics of eQTL and Gene Risk Model and the Inhibitory Effect of DCTD and RRAS on Ferroptosis in Glioblastoma. [Abstract]2025 Aug 30;30(8):42844. PMID: 40917066 -
Breast Cancer Res Treat
Resistance to FOXM1 inhibitors in breast cancer is accompanied by impeding ferroptosis and apoptotic cell death. [Abstract]2024 Nov;208(2):307-320. PMID: 38980505
Lösungsmittel & Löslichkeit
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.
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 10% EtOH 90% PEG400
Solubility: 5 mg/mL (11.08 mM); Clear solution; Need ultrasonic
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (4.43 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Eaton JK, et al. Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles. Nat Chem Biol. 2020;16(5):497-506. [Content Brief]
[2]. Kathman SG, et al. A masked zinger to block GPX4. Nat Chem Biol. 2020;16(5):482-483. [Content Brief]
[3]. Viswanathan VS, et al. Unraveling Masked GPX4 Inhibitors. Nat. Chem. Biol. 2020, 16, 497–506.
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 |
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| 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 |
JKE-1674 Related Classifications
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