- Cat. No.
- A18619
JHU-083
HU-083 is a HU-083 is a Glutamine antagonist, a DON prodrug., a DON prodrug.
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Glutaminase inhibitors block conversion of glutamine to glutamate, the first step of glutaminolysis. The glutaminase 1 (GLS1) gene encodes kidney-type glutaminase (KGA) and its splice variant glutaminase C (GAC), while the glutaminase 2 (GLS2) gene encodes the liver-type enzyme. In 2009 the transcription factor c-Myc was shown to raise mitochondrial glutaminase levels by suppressing two microRNAs. A 2010 study linked mitochondrial glutaminase activity to oncogenic transformation driven by Rho GTPases. Telaglenastat, BPTES and UPGL00004 are allosteric inhibitors of GLS1 enzymes. 6-Diazo-5-oxo-L-norleucine and its prodrug JHU-083 act more broadly as glutamine antagonists. ZED-1227 and GK921 inhibit transglutaminase 2, a distinct enzyme also listed here.
HU-083 is a HU-083 is a Glutamine antagonist, a DON prodrug., a DON prodrug.
Synonyms: Diazooxonorleucine; L-6-Diazo-5-oxonorleucine; DON
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.
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.
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Synonyms: Duazomycin A
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.
Synonyms: Duazomycin A sodium
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.
Synonyms: DRP-104
Sirpiglenastat is a broad-spectrum glutamine antagonist that disrupts tumor metabolism. By targeting glutamine utilization, Sirpiglenastat exhibits significant anticancer effects while simultaneously enhancing the antitumor immune response. This compound is valuable for researchers investigating metabolic pathways in cancer and immune modulation.