FA16 is a specific ferroptosis inducer (IC50=1.26 μM; HT1080 cells) with metabolic stability, is the derivate of 2-(trifluoromethyl)benzimidazole. FA16 acts by inhibiting cystine/glutamate antiporter (system Xc-), which mediates the exchange of intracellular glutamate and extracellular cystine. FA16 significantly inhibits tumor growth in the HepG2 xenograft model.
In Vitro Activity
FA16 (1 μM; 5 min) has satisfactory metabolic stability in rat and human liver microsomes.
FA16 (5 μM; 10 h) induces lipid ROS accumulation and inhibits glutamate release dose-dependently in HT1080 cells.
FA16 (5 μM; 24 h) results mitochondria shrunken with increased membrane density, which was in line with the morphological feature related to ferroptosis.
FA16 (10 μM; 24 h) induced cell death, which can be rescued by the ferroptosis inhibitors Fer-1, Trolox or DFO, but not by the inhibitors of apoptosis or necroptosis.
In Vivo Activity
FA16 significantly inhibits tumor growth with good safety (no weight loss) in 786-O xenograft mice model, and it induced ferroptosis in tumor tissues.
Storage & Handling
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping
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