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 (7):

Cat. No. Product Name Effect Purity
  • HY-12248
    Telaglenastat Inhibitor 99.92%
    Telaglenastat (CB-839) is a potent, selective, and orally bioavailable inhibitor of glutaminase (KGA and GAC) with IC50s of 28 and 23 nM for glutaminase in kidney and brain.
  • HY-12683
    BPTES Inhibitor >98.0%
    BPTES is an allosteric and selective glutaminase inhibitor with an IC50 of 0.16 μM.
  • HY-12682
    Glutaminase C-IN-1 Inhibitor 99.14%
    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-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-122218
    JHU-083 Inhibitor
    JHU-083 selectively blocks glutaminase activity in brain CD11b+ cells. Blocking the function of glutaminase by the glutamine antagonist JHU-083 in experimental cerebral malaria (ECM) can result in a net decrease of glutamate levels in the animals.
  • HY-19359
    ZED-1227 Inhibitor
    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).
  • HY-119377
    UPGL00004 Inhibitor
    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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