Mito-LND

SKU: orb1218348

Description

Mito-LND is an orally active and mitochondria-targeted inhibitor of oxidative phosphorylation.

Key Properties

• CAS Number: 2361564-49-8
• MW: 801.62
• Purity: >98% (HPLC)
• Formula: C₄₃H₄₅BrCl₂N₃OP
• SMILES: O=C(NCCCCCCCCCC[P+](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)C4=NN(CC5=CC=C(Cl)C=C5Cl)C6=C4C=CC=C6.[Br-]
• Target: oxidative phosphorylation (OXPHOS)
• Solubility: DMSO:45mg/ml(56.14mM; need ultrasonic)

Bioactivity

• In Vivo:
  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. Mito-LND also decreases the rate of growth of A549 tumor xenografts. Mito-LND treatment shows a marked decrease in lung cancer brain metastasis in NOD/SCID mice bearing H2030BrM3 cells. Animal model: Athymic nude mice (5 weeks) injected with H2030BrM3 cells. Dosage: 7.5 μmol/kg. Administration: Oral gavage; 5 days per week; for 3 consecutive weeks. Result: Significantly decreased tumor progression.
• In Vitro:
  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. Mito-LND inhibits mitochondrial complex I and II activities with IC50 values of 1.2 μM and 2.4 μM, respectively in H2030BrM3 cells. Mito-LND (1 μM) increases ROS generation in H2030BrM3 lung cancer cells. Mito-LND potently induces mitochondrial ROS generation in H2030BrM3 lung cancer cells. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Mito-Loidamine

Quick Database Links

Gene Symbol

oxidative phosphorylation (OXPHOS)