Glutaminase

ZED-1227 is a specific and oral transglutaminase 2 (TG2) inhibitor, which can block inflammation-induced TG2 expression and activity. ZED-1227 is a promising agent for the treatment of celiac disease (CeD).

CB-839 an is orally bioavailable inhibitor of glutaminase, with potential antineoplastic activity. CB-839 (Telaglenastat) also inudces autophagy and has antitumor activity.

BPTES is a potent and selective Glutaminase GLS1 (KGA) inhibitor with IC50 of 0.16 μM.

HU-083 is a HU-083 is a Glutamine antagonist, a DON prodrug., a DON prodrug.

Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM.

UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC50=29 nM; Kd=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines.

GK921 is a transglutaminase 2 (TGase) inhibitor with an IC50 of 7.71 μM for human recombinant TGase 2.

6-Diazo-5-oxo-L-nor-Leucine is a glutamine antagonist that shows good anticancer activity (especially in pancreatic cancer) and reduces the self-renewal potential and metastatic capacity of tumour cells. 

JFD01307SC is a selective inhibitor of glutamine synthetase, which plays a crucial role in the conversion of L-glutamate to glutamine. By mimicking L-glutamate, JFD01307SC effectively targets and modulates the enzymes involved in glutamine biosynthesis. This compound is primarily utilized in research related to tuberculosis and other metabolic disorders, providing valuable insights into the therapeutic potential of glutamine metabolism modulation.

Azotomycin is an L-glutamine analog that exhibits antitumor activity through the modulation of cellular metabolism and signaling pathways. This compound serves as a valuable tool in cancer research, particularly in studies focusing on glutamine metabolism and its implications in tumor growth and proliferation. Researchers may utilize Azotomycin to investigate therapeutic strategies targeting glutamine-dependent cancer cells.

NSC 303861 is an L-glutamine receptor antagonist that selectively inhibits glutamine-dependent enzymes involved in purine nucleotide synthesis while sparing pyrimidine synthase. This compound exhibits significant cytotoxic effects against liver cancer 3924A cells, with an LC50 of 6 µM. NSC 303861 is valuable for cancer research, particularly in studies focused on targeting metabolic pathways in malignancies.

L-Methionine-DL-sulfoximine is a highly specific and irreversible inhibitor of glutamine synthetase, which significantly affects astroglial metabolism and morphology. This compound also demonstrates potent convulsant properties. L-Methionine-DL-sulfoximine has been utilized in research to inhibit glutamine-dependent neuronal toxicity in vitro and to study the mechanisms underlying convulsive seizures. Additionally, it enhances the rate of fixed nitrogen release in cyanobacteria, making it a valuable tool for applications in biofertilizer research.

Duazomycin is a glutamine antagonist that plays a critical role in modulating metabolic pathways. This compound significantly enhances the efficacy of 6-Mercaptopurine in experimental allergic encephalomyelitis models, demonstrating improved therapeutic outcomes without elevating toxicity. Duazomycin is valuable for research applications focusing on metabolic interactions and therapeutic strategies in autoimmune diseases.

Duazomycin sodium is a potent glutamine antagonist that enhances the efficacy of 6-Mercaptopurine in models of experimental allergic encephalomyelitis (EAE). By targeting glutamine metabolism, it demonstrates potential to improve therapeutic outcomes while maintaining a favorable toxicity profile. This compound is valuable for research applications focused on neuroinflammatory disorders and the modulation of immune responses.