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FerroLOXIN-1 is a potent inhibitor of 15LOX-2 that selectively blocked production of pro-ferroptotic HOO-ETE-PE and protected against RSL3-induced ferroptosis. FerroLOXIN-1 closely interacted therein with 15LOX-2 only, and in particular with Y154, N155, W158[1]. | [Biological Activity]
15LOX/PEBP1 catalytic complex inhibitor th at prevents cell death by ferroptosisbut not necroptosispyroptosisor apoptosis.
FerroLOXIN-1 is a ferroptosis inhibitor th at selectively targets the 15LOX/PEBP1 catalytic complex without affecting the biosynthesis of pro-/anti-inflammatory lipid mediators. FerroLOXIN-1 prevents 0.5 μM GPX4 inhibitor RSL3-induced ferroptosis in HBE cell cultures (IC50 = 84 nM post 20h RSL3 treatment) and rescues mice from total body irradiation (TBI)-induced death in vivo (Cpd administered via 25 mg/kg ip. 20h post 9.25Gy irradiation; survival on day 27 = 75% vs. 0% on day 19 of untreated control). FerroLOXIN-1 does not exert its efficacy via radical scavenging or iron-chelating activitynor does it prevent cell death by necroptosispyroptosisor apoptosis. | [IC 50]
5-LOX | [References]
[1] Dong J, et al. Small Molecule Degraders of Protein Tyrosine Phosphatase 1B and T-Cell Protein Tyrosine Phosphatase for Cancer Immunotherapy. Angew Chem Int Ed Engl. 2023 May 22;62(22):e202303818. |
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