TF-PPAO
TF-PPAO is a blood-brain barrier-penetrant mitochondrial calcium uptake inducer (human Kd = 2.82 μM). TF-PPAO binds the MCUB transmembrane pocket and disrupts MCUB-MCU binding, thereby relieving MCUB-mediated restriction, activating pyruvate dehydrogenase activity, and inducing mitochondrial reactive oxygen species (ROS) and oxidative DNA damage. TF-PPAO acts as a radiosensitizer, inhibits tumor growth, and exhibits intracranial tumor accumulation ability, with no detectable systemic toxicity. TF-PPAO can be used for research on glioblastoma.
For research use only. We do not sell to patients.
- CAS No.: 1424565-75-2
- Formula: C13H11F3N4O
- Molecular Weight:296.25
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Biological Activity
Description
In Vitro
TF-PPAO (serial concentrations; 24 h) inhibits GBM cell viability and has higher IC50 values in HA1800 astrocytes and HUVECs[1].
TF-PPAO (0-8 Gy IR; 14 days) radiosensitizes HG11 and HG23 GBM cells in clonogenic assays, with SER values of 1.30 and 1.35, respectively[1].
TF-PPAO (20 μM; 7 days) restricts the growth of GBO-4 and GBO-6 and enhances IR-mediated growth inhibition[1].
TF-PPAO (40 μM; 24 h) reduces the FRET efficiency of MCUB-eGFP/MCU-mCherry in HG11 cells[1].
TF-PPAO (10-30 μM) dose-dependently disrupts MCUB-MCU co-immunoprecipitation in HG11 and HG23 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:GBM cells, HA1800 astrocytes, and HUVECs
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Concentration:1, 10, 100, 1000 μM
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Incubation Time:24 h
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Result:Inhibited GBM cell viability.
HA1800 astrocytes and HUVECs showed higher IC50 values than GBM cells.
In Vivo
TF-PPAO (60 mg/kg; i.p.; 5 days per week) suppresses intracranial PDX tumor growth and prolongs survival and enhances radiosensitivity when combined with IR[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 4 weeks old)[1]
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Dosage:60 mg/kg
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Administration:i.p.; 5 days per week
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Result:Suppressed intracranial HG11 tumor growth by bioluminescence imaging and prolonged overall survival.
Combination with IR produced the greatest tumor reduction and longest survival.
In intracranial tumors, PDH activity increased and lactate concentration was reduced.
Reduced p-PDHA1 by immunohistochemistry and increased 8-OHdG.
IR combination produced the greatest reduction in Ki-67 and the greatest increase in cleaved caspase-3.
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Animal Model:BALB/c nude (female, 4 weeks old)[1]
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Dosage:60 mg/kg
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Administration:i.p.; 5 days per week
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Result:Suppressed intracranial PDX tumor growth and prolonged survival.
Combination with IR produced the greatest tumor suppression and longest survival.
Increased PDH activity and reduced lactate concentration in PDX tumors.
Reduced p-PDHA1, increased 8-OHdG, reduced Ki-67, and increased cleaved caspase-3, with the strongest effects in the combination group.
Chemical Information
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CAS No. 1424565-75-2
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Molecular Weight 296.25
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Formula C13H11F3N4O
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SMILES
OC(C1)CN1C2=CC(C(F)(F)F)=NC(C3=CC=CN=C3)=N2
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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)
TF-PPAO Related Classifications
HY-191348 Related Classifications
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