Name | JKE-1674 |
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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]. |
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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 |
Density | 1.4±0.1 g/cm3 |
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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 |