- Cart - 0 item(s)
- $0.00
Your shopping cart is empty!
- Chemistry
- Inhibitors
- Natural Products
- Alkaloids
- Amino acid
- Anthraquinones
- Cerebrosides
- Chalcones
- Coumarins
- Diterpenoids
- Flavonoids
- Iridoids
- Lignans
- Lipids
- Miscellaneous
- Monoterpenoids
- Other terpenes
- Phenols
- Phenylpropanoids
- Quinones
- Saccharides
- Sesquiterpenoids
- Steroids
- Tetraterpenoids
- Thiophenes
- Triterpenoids
- Xanthones
- Polyphenols
- Stibene glucosides
- Oligose
- Anthocyanins
- Miscellaneous
- Chromones
- Terpenoids
- Indoles
- Procyanidins
- Aliphatics
- Botanical Cyclopeptides
- ADCs
- Antibodies
- Multiplex IHC
- Material Science
- Others
[CAS NO. 2421119-60-8] JKE-1674
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-138153 |
| Brand: | MCE |
| CAS: | 2421119-60-8 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 451.30 |
| Molecular Formula | C20H20Cl2N4O4 |
| 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 |
Summary
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] .
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] .
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. |
Appearance
Solid
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
DMSO : 100 mg/mL ( 221.58 mM ; Need ultrasonic)
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 |
| 10 mM | 0.2216 mL | 1.1079 mL | 2.2158 mL |
References
- [1] Eaton JK, et al. Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles. Nat Chem Biol. 2020;16(5):497-506.
- [2] Kathman SG, et al. A masked zinger to block GPX4. Nat Chem Biol. 2020;16(5):482-483.
- [3] Viswanathan VS, et al. Unraveling Masked GPX4 Inhibitors. Nat. Chem. Biol. 2020, 16, 497–506.
Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.