1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. 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.

Glutaminase Related Products (10):

Cat. No. Product Name Effect Purity
  • HY-12248
    Telaglenastat Inhibitor 99.92%
    Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat 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. Telaglenastat inudces autophagy and has antitumor activity.
  • HY-12683
    BPTES Inhibitor 98.07%
    BPTES is an allosteric and selective glutaminase inhibitor with an IC50 of 0.16 μM.
  • HY-108357
    6-Diazo-5-oxo-L-nor-Leucine Antagonist >99.0%
    L-6-Diazo-5-oxonorleucine (L-6-Diazo-5-oxonorleucine) is a glutaminases antagonist with a Ki of 6 μM. L-6-Diazo-5-oxonorleucine exhibits analgesic, antibacterial, antiviral and anticancer properties. L-6-Diazo-5-oxonorleucine displays genetic toxicity in vitro. L-6-Diazo-5-oxonorleucine decreases the self-renewal potential and metastatic ability of tumor cell.
  • HY-12682
    Glutaminase C-IN-1 Inhibitor 99.61%
    Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.
  • HY-122218
    JHU-083 Antagonist
    JHU-083, a prodrug of 6-diazo-5-oxo-L-norleucine (DON; HY-108357), is an orally active and selective glutaminase antagonist. JHU-083 blocks glutaminase activity in brain CD11b+ cells and experimental cerebral malaria (ECM) resulting in a net decrease of glutamate levels in the animals.
  • HY-103671A
    IPN-60090 dihydrochloride Inhibitor
    IPN-60090 dihydrochloride is an orally bioavailable and selective inhibitor of GLS1 (the kidney-type glutaminase), an important enzyme for metabolic energy production. IPN-60090 dihydrochloride can be used in the research of GLS1-mediated diseases.
  • HY-114334
    Glutaminase-IN-1 Inhibitor 98.05%
    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.
  • HY-12337
    GK921 Inhibitor 99.92%
    GK921 is a transglutaminase 2 (TGase) inhibitor with an IC50 of 7.71 μM for human recombinant TGase 2.
  • HY-19359
    ZED-1227 Inhibitor 99.97%
    ZED-1227 is a specific and oral transglutaminase 2 (TG2) inhibitor, with an IC50 of 45 nM. ZED-1227 can block inflammation-induced TG2 expression and activity. ZED-1227 can be used for the research of celiac disease (CeD).
  • HY-119377
    UPGL00004 Inhibitor >98.0%
    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.
Isoform Specific Products

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