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)^[1].

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.

Glutaminase C-IN-3 (compound 16) (10 and 30 mg/kg, i.p., daily for 22 days) exhibits antitumor efficacy in an A549 xenograft mouse model with good safety^[1].

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

656.68

C₃₁H₃₁F₃N₆O₅S

3120156-36-4

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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• [1]. Sun H, et al. Structure-enabled discovery of carboxylate esters prodrugs as potential potent inhibitors targeting Glutaminase C. Bioorg Chem. Published online November 24, 2025.  [Content Brief]