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JKE-1674

Cat. No. M10586
JKE-1674 Structure
Synonym:

JKE1674

Size Price Availability Quantity
2mg USD 130  USD130 In stock
5mg USD 320  USD320 In stock
10mg USD 490  USD490 In stock
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Quality Control & Documentation
Biological Activity

JKE-1674 is an inhibitor of glutathione peroxidase 4 (GPX4) and an active metabolite of the GPX4 inhibitor ML-210. JKE-1674 reduces viability of LOX-IMVI cancer cells and in a panel of additional cancer cell lines, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1. 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.

Chemical Information
Molecular Weight 451.30
Formula C20H20Cl2N4O4
CAS Number 2421119-60-8
Solubility (25°C) DMSO 90 mg/mL
Storage 2-8°C, protect from light, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] John K Eaton, et al. Nat Chem Biol. Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles

[2] Stefan G Kathman, et al. Nat Chem Biol. A masked zinger to block GPX4

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Keywords: JKE-1674, JKE1674 supplier, Ferroptosis, inhibitors, activators


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