JKE-1674
- Product Name
- JKE-1674
- CAS No.
- 2421119-60-8
- Chemical Name
- JKE-1674
- Synonyms
- JKE-1674;JKE-1674, 10 mM in DMSO;JKE-1674 (mixture of isomers);1-[4-[Bis(4-chlorophenyl)methyl]-1-piperazinyl]-3-nitro-1,2-propanedione 2-oxime;1,2-Propanedione, 1-[4-[bis(4-chlorophenyl)methyl]-1-piperazinyl]-3-nitro-, 2-oxime;(E)-1-(4-(bis(4-chlorophenyl)methyl)piperazin-1-yl)-2-(hydroxyimino)-3-nitropropan-1-one;ML210,glutathione,Ferroptosis,JKE-1674,peroxidase,inhibit,JKE 1674,Glutathione Peroxidase,rescued,Inhibitor,JKE1674
- CBNumber
- CB46197997
- Molecular Formula
- C20H20Cl2N4O4
- Formula Weight
- 451.3
- MOL File
- 2421119-60-8.mol
JKE-1674 Property
- Boiling point:
- 595.5±60.0 °C(Predicted)
- Density
- 1.43±0.1 g/cm3(Predicted)
- storage temp.
- 4°C, protect from light
- solubility
- DMSO: soluble
- form
- A crystalline solid
- pka
- 6.67±0.58(Predicted)
- color
- Off-white to light yellow
- InChI
- InChI=1S/C20H20Cl2N4O4/c21-16-5-1-14(2-6-16)19(15-3-7-17(22)8-4-15)24-9-11-25(12-10-24)20(27)18(23-28)13-26(29)30/h1-8,19,28H,9-13H2
- InChIKey
- XIOHKIAPXVDWCP-UHFFFAOYSA-N
- SMILES
- C(N1CCN(C(C2=CC=C(Cl)C=C2)C2=CC=C(Cl)C=C2)CC1)(=O)C(=NO)C[N+]([O-])=O
JKE-1674 Chemical Properties,Usage,Production
Uses
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].
Biological Activity
JKE-1674 is an inhibitor of glutathione peroxidase 4 (GPX4) and an active metabolite of the GPX4 inhibitor ML-210 .1 JKE-1674 reduces viability of LOX-IMVI cancer cells (EC50 = 0.03 μM) and in a panel of additional cancer cell lines, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1 .
in vivo
JKE-1674 (50mg/kg; p.o.) can be detected in the serum of mice dosed orally with the compound[1].
| Animal Model: | SCID mice[1] |
| Dosage: | 50mg/kg (Pharmacokinetic Analysis) |
| Administration: | P.o. |
| Result: | Could be detected in the serum of mice dosed orally with the compound. |
References
1.Eaton, J.K., Furst, L., Ruberto, R.A., et al.Selective covalent targeting of GPX4 using masked nitrile-oxide electrophilesNat. Chem. Biol.16(5)497-506(2020)
JKE-1674 Preparation Products And Raw materials
Raw materials
Preparation Products
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