MDL | - |
---|---|
Molecular Weight | 1074.05 |
Molecular Formula | C65H64Cl2O6P2 |
SMILES | O=C(C(C(/C=C/C1=CC=C(OCCC[P+](C2=CC=CC=C2)(C3=CC=CC=C3)C4=CC=CC=C4)C(OC)=C1)=O)(C)C)/C=C/C5=CC(OC)=C(OCCC[P+](C6=CC=CC=C6)(C7=CC=CC=C7)C8=CC=CC=C8)C=C5.[Cl-].[Cl-] |
MitoCur-1, a curcumin analogue, is an inhibitor of mitochondrial antioxidative thioredoxin reductase 2 (TrxR2) . MitoCur-1 has electrophilic and mitochondrial-targeting properties. MitoCur-1 induces reactive oxygen species (ROS) generation, exerts specifically antitumor efficacy [1] .
Thioredoxin reductase 2 (TrxR2) [1]
MitoCur-1 exhibits selective cytotoxicity against HepG2 and L02 cells with IC50s of 1.4 μM and 9.1 μM, respectively
[1]
.
MitoCur-1 (10 μM; 12 h) generates ROS and depletes GSH selectively in HepG2 cells over L02 cells
[1]
.
MitoCur-1 (10 μM; 24 h) arrests cell cycle at G0/G1 phase, inhibits cyclin protein expression
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
Cell Line: | HepG2 cells |
Concentration: | 2.5 μM, 5 μM, and 10 μM |
Incubation Time: | 24 h, 36 h, and 48 h |
Result: | Decreased the protein level of CDK2 and CDK4, Cyclin E1/D1/A2. |
Immunofluorescence [1]
Cell Line: | HepG2 and L02 cells |
Concentration: | 10 μM |
Incubation Time: | 12 h |
Result: | Showed selectivity on HepG2 cells over L02 cells to generates ROS. Promoted mitochondrial O 2 - production. |
Cell Viability Assay [1]
Cell Line: | HepG2 cells |
Concentration: | 1.25 μM, 2.5 μM, 5 μM, and 10 μM |
Incubation Time: | 48 h; pretreated with 400 μM DTT or not |
Result: | Inhibited HepG2 cells viability. Showed significant reversion with DTT for 1 h pretreatment. |
MitoCur-1 (5 mg/kg, 15 mg/kg; i.p.; every other day for 4 weeks) inhibits tumor growth in mouse model without effect on body weight [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | BALB/c nude mice bearing HepG2 tumor [1] |
Dosage: | 5 mg/kg, 15 mg/kg |
Administration: | Intraperitoneal injection; every other day for 4 weeks |
Result: | Decreased the tumor growth in vivo. |
Room temperature in continental US; may vary elsewhere.
Please store the product under the recommended conditions in the Certificate of Analysis.