OXPHOS-IN-2
OXPHOS-IN-2 is an orally active OXPHOS inhibitor. OXPHOS-IN-2 exhibits potent inhibitory activity in PC9 (IC50 = 12.3 nM) and Bxpc-3 cells (IC50 = 250 nM in glucose medium, IC50 = 17.5 nM in galactose medium). OXPHOS-IN-2 decreases the NADH/NAD+ ratio and reduces ATP levels. OXPHOS-IN-2 induces tumor cells apoptosis by activating reactive oxygen species (ROS) and downregulating the level of Nrf2. OXPHOS-IN-2 can be used for research on cancer such as non-small cell lung cancer and pancreatic cancer.
For research use only. We do not sell to patients.
- Formula: C27H27F3N6O4S
- Molecular Weight:588.60
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All AMPK Isoforms
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Biological Activity
OXPHOS-IN-2 (Compound 28c) (0-1000 μM, 12 h) reduces the ratio of ATP and NAD+/NADH and inhibits AMPK phosphorylation in PC9 cells[1].
OXPHOS-IN-2 (0-20 nM, 14 days) significantly inhibits the colony forming ability of PC9 cells[1].
OXPHOS-IN-2 (0-1 μM) can induce apoptosis by dose dependently increasing reactive oxygen species (ROS) levels and reducing mitochondrial membrane potential in PC9 and Bxpc-3 cells[1].
OXPHOS-IN-2 (0-50 nM) induces DNA damage and increases the expression of γ-H2AX in PC9 cells[1].
OXPHOS-IN-2 can inhibit the proliferation of various tumor cell lines in glucose and galactose medium, including H1975 (IC50 = 6.43 nM and 29.5 nM), H2228 (IC50 = 4.54 nM and 21.5 nM), KP-4 (IC50 = 3.61 nM and 48.7 nM), MKN45 (IC50 = 5.78 nM and 29.8 nM), HCT116 (IC50 = 5.19 nM and 31.2 nM), MDA-MB-231 (IC50 = 1.31 nM and 7.5 nM), MHCC-97H (IC50 = 1.76 nM and 12.4 nM) and SiHA (IC50 = 5.10 nM and 35.1 nM) cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC9 spheres
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Concentration:1, 10, 20 nM
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Incubation Time:72 h
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Result:Significantly increased the apoptosis rate of cells.
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Cell Line:PC9 cells
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Concentration:1, 10, 50 nM
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Incubation Time:12 h
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Result:Significantly reduced the level of pAMPK.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5×107 PC9 cells injected male BALB/c-nu mice (3-4 weeks)[1]
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Dosage:7.5 mg/kg
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Administration:Oral administration (p.o.); once daily for 14 days
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Result:Significantly inhibited tumor volume and tumor weight, superior to IACS-010759 (HY-112037).
Did not cause significant changes in weight.
Significantly reduced NAD+/NADH ratio and ATP content.
Chemical Information
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Molecular Weight 588.60
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Formula C27H27F3N6O4S
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SMILES
FC(F)(F)OC1=CC=C(C2=NOC(C3=NN(CC4=CC=CC(N5CCC(S(=O)(C)=O)CC5)=C4)C(C6CC6)=N3)=N2)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)