2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
CAS NO.：2421119-60-8 Product Name：(E)-1-(4-(bis(4-chlorophenyl)methyl)piperazin-1-yl)-2-(hydroxyimino)-3-nitropropan-1-one Synonyms：(E)-1-(4-(bis(4-chlorophenyl)methyl)piperazin-1-yl)-2-(hydroxyimino)-3-nitropropan-1-one;(2E)-1-[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]-2-hydroxyimino-3-nitropropan-1-one;JKE-1674 EINEC: Molecular Formula：C20H20CL2N4O4 Molecular Weight：451.303202629089
Target:
GPX4[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.
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].
Kinase Assay
Cell Assay
Animal Administration
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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