Mito-LND (Synonyms: Mito-Lonidamine) |
رقم الكتالوجGC62564 |
Mito-LND (Mito-Lonidamine) هو مثبط نشط عن طريق الفم ويستهدف الميتوكوندريا من الفسفرة المؤكسدة (OXPHOS)يثبط Mito-LND الطاقة الحيوية للميتوكوندريا ، ويحفز تكوين أنواع الأكسجين التفاعلية ، ويحث على موت خلايا البلعمة الذاتية في خلايا سرطان الرئة
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Cas No.: 2361564-49-8
Sample solution is provided at 25 µL, 10mM.
Mito-LND (Mito-Lonidamine) is an orally active and mitochondria-targeted inhibitor of oxidative phosphorylation (OXPHOS). Mito-LND inhibits mitochondrial bioenergetics, stimulates the formation of reactive oxygen species, and induces autophagic cell death in lung cancer cells[1].
Mito-LND blocks lung cancer growth, migration, and invasion. Mito-LND inhibits cell growth of H2030BrM3 and A549 cells with IC50 values of 0.74 µM and 0.69 µM, respectively[1].Mito-LND inhibits mitochondrial complex I and II activities with IC50 values of 1.2 µM and 2.4 µM, respectively in H2030BrM3 cells[1]. Mito-LND (1 µM) increases ROS generation in H2030BrM3 lung cancer cells. Mito-LND potently induces mitochondrial ROS generation in H2030BrM3 lung cancer cells[1].Mito-LND (2 µM) decreases the levels of phosphorylated AKT. Mito-LND also decreases the phosphorylation of P70S6K and other energy-sensing proteins in both the parental and metastatic lung cancer cell lines, indicating that Mito-LND specifically downregulates mTOR signaling[1].
Mito-LND (7.5 µmol/kg; oral gavage; 5 days per week; for 3 consecutive weeks) treatment markedly enhanced potency against both lung cancer progression and metastasis[1]. Mito-LND also decreases the rate of growth of A549 tumor xenografts[1].Mito-LND treatment shows a marked decrease in lung cancer brain metastasis in NOD/SCID mice bearing H2030BrM3 cells[1].
[1]. Gang Cheng, et al. Targeting lonidamine to mitochondria mitigates lung tumorigenesis and brain metastasis. Nat Commun. 2019 May 17;10(1):2205.
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