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.
|Solubility (25°C)||DMSO 90 mg/mL|
|Storage||2-8°C, protect from light, sealed|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Related Ferroptosis Products|
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Piperazine Erastin is an Erastin derivative and an inducer of ferroptosis.
N6F11 is a novel ferroptosis inducer that selectively triggers the ubiquitination degradation of GPX4 by binding to the specific structural domain of TRIM25, a ubiquitinated E3 ligase, which is expressed in tumor cells, leading to ferroptosis in cancer cells.
FSEN1 is a potent and non-competitive FSP1 inhibitor with an IC50 value of 313 nM.
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