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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
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 451.30
Formula C20H20Cl2N4O4
CAS Number 2421119-60-8
Purity >98%
Solubility DMSO 90 mg/mL
Storage 2-8°C, protect from light, sealed
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

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