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