Home >> Signaling Pathways >> Proteases >> Glutaminase

Glutaminase

Glutaminase is an amidohydrolase enzyme that generates glutamate from glutamine. Glutamate production by mitochondrial glutaminase is a key process for body homeostasis, and a crucial carbon donor for amino acid and lipid synthesis in tumor cells.

Glutaminase has tissue-specific isoenzymes. Three mammalian glutaminases have been identified: the liver-type [LGA or GLS2], the kidney-type [KGA] and Glutaminase C [GAC] a splice variant of KGA (both usually referred to as GLS1). GLS1 is a therapeutic target for cancer. GLS1 catalyzes the hydrolysis of glutamine to glutamate, which is used in the citric acid cycle (TCA) of cancer cells undergoing an aberrant glycolytic flux as a non-glucose-derived source for anaplerosis. GAC plays an essential role in the transformation of NIH 3T3 fibroblasts by Rho GTPases, as well as in the proliferative and invasive activities of various cancer cells.

Targets for  Glutaminase

Products for  Glutaminase

  1. Cat.No. Product Name Information
  2. GC66717 2-Amino-2-(p-tolyl)acetic acid 2-Amino-2-(p-tolyl)acetic acid is used for optimizing azide skeleton, and is the intermediate in the synthesis of 1,3, 4-thiadiazole compounds. 1,3,4-thiadiazole compounds exhibit potential anti-cancer activity, and inhibit glutaminase (GLSI). 2-Amino-2-(p-tolyl)acetic acid  Chemical Structure
  3. GC41224 6-diazo-5-oxo-L-nor-Leucine

    6-Diazo-5-oxo-L-nor-Leucine (DON) is a glutamine analog that inhibits glutaminases, a selective, mechanism-based inactivator of glutamine-using enzymes[1-3].

    6-diazo-5-oxo-L-nor-Leucine  Chemical Structure
  4. GC13958 BPTES A GLS inhibitor BPTES  Chemical Structure
  5. GC15227 CB-839 CB-839 (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. CB-839 selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. CB-839 inudces autophagy and has antitumor activity. CB-839  Chemical Structure
  6. GC67898 GLS-1-IN-1 GLS-1-IN-1  Chemical Structure
  7. GC19171 Glutaminase C-IN-1 Glutaminase C-IN-1 (968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts. Glutaminase C-IN-1  Chemical Structure
  8. GC33274 Glutaminase-IN-1 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. Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity. Glutaminase-IN-1  Chemical Structure
  9. GC62285 Glutaminase-IN-3 SRS11-92, a Ferrostatin-1 (Fer-1) analogue, is a potent ferroptosis inhibitor. SRS11-92 inhibits ferroptotic cell death induced by Erastin in HT-1080 human fibrosarcoma cells (EC50=6 nM). Glutaminase-IN-3  Chemical Structure
  10. GC62618 IPN60090 IPN-60090 is an orally active and highly selective inhibitor of glutaminase 1?(GLS1; IC50=31 nM), with no activity observed against GLS-2. IPN60090  Chemical Structure
  11. GC36368 JHU-083 JHU-083, a prodrug of 6-diazo-5-oxo-L-norleucine is an orally active and selective glutaminase antagonist. JHU-083  Chemical Structure
  12. GC25536 JHU395 JHU395 is a novel orally bioavailable GA (glutamine antagonists) prodrug designed to circulate inert in plasma, but permeate and release active GA within target tissues. JHU395 delivers active GA to malignant peripheral nerve sheath tumor (MPNST), and significantly inhibits tumor growth without observed toxicity. JHU395  Chemical Structure
  13. GC64531 KCC009 KCC009, a transglutaminase 2 (TG2) inhibitor, induces p53-independent radiosensitization. KCC009  Chemical Structure
  14. GC70020 TG-2-IN-1

    TG-2-IN-1 (Compound D003) is a transglutaminase-2 (TGM-2) inhibitor. TG-2-IN-1 can be used for myopia research.

    TG-2-IN-1  Chemical Structure
  15. GC37963 ZED-1227 ZED-1227 is a specific and orally active transglutaminase 2 (TG2) inhibitor, with an IC50 of 45 nM. ZED-1227  Chemical Structure

14 Item(s)

per page

Set Descending Direction