1. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Autophagy Apoptosis PI3K/Akt/mTOR
  2. Reactive Oxygen Species (ROS) Mitochondrial Metabolism Mitophagy Apoptosis PI3K Akt mTOR
  3. Molephantin

Molephantin is a blood-brain barrier permeable anti-glioblastoma compound. Molephantin induces ROS generation, leading to mitochondrial damage, Mitophagy flux blockage and Apoptosis induction. Molephantin can suppress the PI3K/Akt/mTOR signaling pathway. Molephantin demonstrates antitumor effects against glioblastoma.

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Molephantin

Molephantin Chemical Structure

CAS No. : 50656-66-1

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Description

Molephantin is a blood-brain barrier permeable anti-glioblastoma compound. Molephantin induces ROS generation, leading to mitochondrial damage, Mitophagy flux blockage and Apoptosis induction. Molephantin can suppress the PI3K/Akt/mTOR signaling pathway. Molephantin demonstrates antitumor effects against glioblastoma[1].

In Vitro

Molephantin (72 h) inhibits proliferation of U251 and U87 glioblastoma cells with IC50 values of 10.58 μM and 22.64 μM, respectively[1].
Molephantin (1-10 μM; 6-24 h) suppresses the PI3K/Akt/mTOR signaling pathway in U251 and U87 glioblastoma cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: U251, U87
Concentration: 5-10 μM
Incubation Time: 24 h
Result: Arrested the cell cycle in the S phase, decreasing the proportion of cells in the G0/G1 phase and increasing the proportion in the S phase

Western Blot Analysis[1]

Cell Line: U251, U87
Concentration: 1-10 μM
Incubation Time: 6-24 h
Result: Decreased p-PI3K, p-Akt, and p-mTOR expression; reversed by NAC
In Vivo

Molephantin (10-30 mg/kg; i.p.; every two days; 21 days) significantly inhibits glioblastoma growth in BALB/c nude mice bearing U87 xenografts without obvious toxic effects[1].
Molephantin (30 mg/kg; i.p.) penetrates the blood-brain barrier in *C57BL/6* mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice (female, 7 weeks old)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: i.p.; every two days; until day 21 post-administration
Result: Decreased tumor volume significantly; Reduced mean tumor weight to 0.17±0.05 g (10 mg/kg) and 0.12±0.07 g compared to control; Increased expression of apoptosis-related proteins (cleaved caspase 9, cleaved caspase 7, cleaved caspase 3, cleaved PARP) in tumor tissues; Increased Cleaved caspase 3-positive cells and TUNEL-positive cells; Decreased Ki67-positive cells.
Animal Model: C57BL/6 mice (male, 20–22 g)[1]
Dosage: 30 mg/kg
Administration: i.p.
Result: Detected a high chromatographic peak matching the Molephantin standard sample at 3.76 min in both plasma and brain tissue samples, confirming penetration through the blood-brain barrier.
Molecular Weight

346.37

Formula

C19H22O6

CAS No.
SMILES

[H][C@@](C1=C)([C@@H](OC(C(C)=C)=O)C/C(C)=C\2)[C@]([C@@H](O)/C(C)=C\C2=O)([H])OC1=O

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