2421119-60-8

2421119-60-8 structure
2421119-60-8 structure
  • Name: JKE-1674
  • Chemical Name: JKE-1674
  • CAS Number: 2421119-60-8
  • Molecular Formula: C20H20Cl2N4O4
  • Molecular Weight: 451.303
  • Catalog: Signaling Pathways Apoptosis Ferroptosis
  • Create Date: 2021-08-15 18:02:45
  • Modify Date: 2024-01-10 14:24:06
  • JKE-1674 is an orally active glutathione peroxidase 4 (GPX4) inhibitor. JKE-1674 kills cells in a manner that is equipotent to ML210 and is completely rescued by ferroptosis inhibitors[1].

Name JKE-1674
Synonyms 1,2-Propanedione, 1-[4-[bis(4-chlorophenyl)methyl]-1-piperazinyl]-3-nitro-, 2-oxime, (2E)-
(2E)-1-{4-[Bis(4-chlorophenyl)methyl]-1-piperazinyl}-2-(hydroxyimino)-3-nitro-1-propanone
JKE-1674
Description JKE-1674 is an orally active glutathione peroxidase 4 (GPX4) inhibitor. JKE-1674 kills cells in a manner that is equipotent to ML210 and is completely rescued by ferroptosis inhibitors[1].
Related Catalog
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 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].
In Vivo JKE-1674 (50 mg/kg; p.o.) can be detected in the serum of mice dosed orally with the compound[1]. 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.
References

[1]. Eaton JK, et al. Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles. Nat Chem Biol. 2020;16(5):497-506.

Density 1.4±0.1 g/cm3
Boiling Point 595.5±60.0 °C at 760 mmHg
Molecular Formula C20H20Cl2N4O4
Molecular Weight 451.303
Flash Point 313.9±32.9 °C
Exact Mass 450.086151
LogP 3.35
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.651