Mito-LND (Mito-Lonidamine) 是一种具有口服活性的且靶向线粒体的氧化磷酸化 (oxidative phosphorylation (OXPHOS)) 抑制剂。Mito-LND 抑制线粒体生物能，刺激活性氧 (reactive oxygen species) 的形成，并诱导肺癌细胞自噬细胞死亡。
货号:ajcx33972
CAS:2361564-49-8
分子式:C43H45BrCl2N3OP
分子量：801.62
溶解度:DMSO : 50 mg/mL (62.37 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.