Glutaminase C-IN-3
Glutaminase C-IN-3 is a potent allosteric inhibitor of Glutaminase C (GAC) with an EC50 of 116 nM. Glutaminase C-IN-3 regulates cellular metabolites and increases reactive oxygen species (ROS) production by blocking glutamine metabolism. Glutaminase C-IN-3 exhibits strong antitumor activity in an A549 xenograft mouse model. Glutaminase C-IN-3 can be used for the research of non-small cell lung cancer (NSCLC).
For research use only. We do not sell to patients.
- CAS No.: 3120156-36-4
- Formula: C31H31F3N6O5S
- Molecular Weight:656.68
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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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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
GAC 116 nM (EC50) |
In Vitro
Glutaminase C-IN-3 (compound 16) (72 h) demonstrates potent antiproliferative activity in A549 cells (IC50 = 2.45 nM), while showing selectivity over normal cells (BEAS-2B) with an IC50 of 1.12 µM[1].
Glutaminase C-IN-3 (30-300 nM, 16 h) significantly disrupts glutamine metabolism, leading to a concentration-dependent reduction in the glutamate/glutamine ratio in A549 cells[1].
Glutaminase C-IN-3 (300 nM-1 µM, 16 h) induces a dose-dependent increase in ROS levels in A549 cells, indicating enhanced ROS generation and a loss of redox homeostasis[1].
Glutaminase C-IN-3 (5 μM, 1 h) demonstrates high stability in simulated gastric fluid(SGF) and simulated intestinal fluid (SIF)[1].
Glutaminase C-IN-3 (5 µM, 0.25-2 h) exhibits moderate metabolic stability in rat liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Balb/c nude mice inoculated with A549 tumor fragments[1]
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Dosage:10 and 30 mg/kg
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Administration:i.p., once daily for 22 days
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Result:Showed tumor growth inhibition with a TGI of 25.8% at 10 mg/kg.
Did not significantly enhance efficacy at 30 mg/kg.
Showed no significant body weight decrease.
Chemical Information
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CAS No. 3120156-36-4
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Molecular Weight 656.68
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Formula C31H31F3N6O5S
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SMILES
O=C(OC(C)C)C1=CC=CC(CC(NC2=NN=C(CCCCC3=NN=C(NC(CC4=CC=CC(OC(F)(F)F)=C4)=O)C=C3)S2)=O)=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)
Glutaminase C-IN-3 Related Classifications
HY-180241 Related Classifications
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