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JKE-1674
Cat. No. IC23208
CAS. No. 2421119-60-8
Key Features and Details
Category
Inhibitor&Activator
Purity
0.9801
Formula
C20H20Cl2N4O4
Product Details
Product Name
JKE-1674
CAS No.
2421119-60-8
Molecular Weight
451.3
Target
GPX4
Formula
C20H20Cl2N4O4
Appearance
Solid
Purity
0.9801
SMILES
O=C(N1CCN(C(C2=CC=C(Cl)C=C2)C3=CC=C(Cl)C=C3)CC1)/C(C[N+]([O-])=O)=N/O
Product Overview
Description
JKE-1674 is an orally active glutathione peroxidase 4 (GPX4) inhibitor and an active metabolite of GPX4 inhibitor ML-210. JKE-1674, an analog of ML-210 in which the nitroisoxazole ring is replaced with an α-nitroketoxime. JKE-1674 can convert into a nitrile oxide JKE-1777. JKE-1674 kills LOX-IMVI cells in a manner that is equipotent to ML-210 and is completely rescued by ferroptosis inhibitors.
In Vitro Activity
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 LOX-IMVI 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 Activity
JKE-1674 can be detected in the serum of mice dosed orally with the compound.
Storage & Handling
Storage
4 °C, protect from light
In solvent : -80 °C, 6 months; -20 °C, 1 month (protect from light)
Shipping
Room temperature in continental US; may vary elsewhere.
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