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.
Product information
CAS Number: 2421119-60-8
Molecular Weight: 451.30
Formula: C20H20Cl2N4O4
Chemical Name: (2E)-1-{4-[bis(4-chlorophenyl)methyl]piperazin-1-yl}-2-(N-hydroxyimino)-3-nitropropan-1-one
Smiles: [O-][N+](=O)C/C(=N\O)/C(=O)N1CCN(CC1)C(C1C=CC(Cl)=CC=1)C1C=CC(Cl)=CC=1
InChiKey: XIOHKIAPXVDWCP-PTGBLXJZSA-N
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/b23-18+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (221.58 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
In Vivo:
JKE-1674 (50 mg/kg; p.o.) can be detected in the serum of mice dosed orally with the compound.
Products are for research use only. Not for human use.
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