2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Glutaminase

Glutaminase

Glutaminase

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Glutaminase is the initial enzyme in glutamine metabolism, which catalyzes the hydrolysis of glutamine to glutamate in cells. Glutaminase plays a key role in cancer cell metabolism, growth, and proliferation. In mammalian cells, there are two paralogous GLS genes, GLS1 (or GLS) and GLS2. GLS1 encodes two alternatively spliced isozymes: kidney glutaminase (KGA) and glutaminase C (GAC). GLS2 also encodes two isozymes: liver glutaminase (LGA) and glutaminase B.

GLS1 is ubiquitously expressed in various tissues, and its expression can be induced by the oncogene MYC. GLS1 is frequently activated and/or overexpressed in various types of cancer, including hepatocellular carcinoma (HCC). GLS1 has been reported to promote tumorigenesis in different types of cancer, including HCC, which is mainly attributable to its glutaminase activity and role in promoting glutamine metabolism. GLS has emerged as a critical enzyme in a number of cancer types. Elevated GLS2 enzymatic activity has also been correlated with tumor cell growth in vitro and in vivo. N-Myc activates GLS2 to promote conversion of glutamine to glutamate in MYCN-amplified neuroblastoma cells. Abrogation of GLS2 function profoundly inhibits glutaminolysis and dramatically decreases cell proliferation and survival in vitro and in vivo. However, there is controversy over the role of GLS2 as a tumor suppressor. Enzymatic activity independent of GLS2 is up-regulated via p53 or p63 and plays a role of tumor suppressor.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-12248
    Telaglenastat
    		Inhibitor 99.82%
    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 inuduces autophagy and has antitumor activity.
    Telaglenastat
  • HY-12683
    BPTES
    		Inhibitor 98.75%
    BPTES is an allosteric and selective glutaminase inhibitor with an IC50 of 0.16 μM.
    BPTES
  • HY-108357
    6-Diazo-5-oxo-L-nor-Leucine
    		Antagonist 99.98%
    6-Diazo-5-oxo-L-nor-Leucine (L-6-Diazo-5-oxonorleucine; DON) is a glutamine antagonist that irreversibly inhibits the catabolic effect of glutamine. 6-Diazo-5-oxo-L-nor-Leucine shows good anticancer activity (especially in pancreatic cancer) and reduces the self-renewal potential and metastatic capacity of tumour cells. 6-Diazo-5-oxo-L-nor-Leucine also possesses antibacterial and antiviral activity.
    6-Diazo-5-oxo-L-nor-Leucine
  • HY-B1692
    L-Methionine-DL-sulfoximine
    		Inhibitor ≥98.0%
    L-Methionine-DL-sulfoximine (MSX; MSO), a highly specific and irreversible inhibitor of Glutamine synthetase (GS), is also a potent convulsant which metabolically and morphologically primarily affects astroglia. L-Methionine-DL-sulfoximine has been employed to inhibit the Gln-dependent ammonia-stimulated neuronal toxicity in vitro, potentiating Gln deficit-dependent depression. L-Methionine-DL-sulfoximine tremendously increases the rate of release of fixed nitrogen in cyanobacteria. L-Methionine-DL-sulfoximine is a promising candidate for research in biofertilizers and convulsive seizures (CS).
    L-Methionine-DL-sulfoximine
  • HY-12337
    GK921
    		Inhibitor 99.91%
    GK921 is a transglutaminase 2 (TGase) inhibitor with an IC50 of 7.71 μM for human recombinant TGase 2.
    GK921
  • HY-W353728
    N-Carbobenzoxytyramine
    		Inhibitor 98.62%
    N-Carbobenzoxytyramine (N-CBZ-Tyramine), a carbobenzoxy derivatives of amino acid, is a competitive inhibitor of glutaminase activity.
    N-Carbobenzoxytyramine
  • HY-180322
    TG2-IN-3h
    		Inhibitor
    TG2-IN-3h (Compound 3h) is a transglutaminase (TG2) inhibitor (hTG2: IC50 = 6nM). TG2-IN-3h inhibits endothelial cell migration and angiogenesis. TG2-IN-3h alleviates renal fibrosis in a mouse model of hypertensive nephropathy. TG2-IN-3h can be used in research on metabolic diseases such as hypertensive nephropathy and cardiovascular and cerebrovascular diseases such as pathological angiogenesis.
    TG2-IN-3h
  • HY-181890
    TRG-192
    		Inhibitor
    TRG-192 is a potent and selective glutaminase (GLS) inhibitor with an IC50 of 68 nM. TRG-192 inhibits intracellular glutamate levels. TRG-192 is applicable to related research on non-small cell lung cancer.
    TRG-192
  • HY-122218
    JHU-083
    		Antagonist 99.38%
    JHU-083, a proagent 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.
    JHU-083
  • HY-W015309
    Decanoic acid
    		Inhibitor 98.0%
    Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy.
    Decanoic acid
  • HY-124476
    Cystamine
    		Inhibitor 99.85%
    Cystamine is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD) .
    Cystamine
  • HY-16693
    LDN-27219
    		Inhibitor 99.76%
    LDN-27219 is a reversible, slow-binding inhibitor of TGase. LDN-27219 inhibits human TGase with an IC50 value of 0.6 μM. LDN-27219 effectively decreases blood pressure and induces vasodilation, it can be used for the research of cardiovascular disease.
    LDN-27219
  • HY-12682
    Glutaminase C-IN-1
    		Inhibitor 99.89%
    Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.
    Glutaminase C-IN-1
  • HY-19359
    Vilagletistat
    		Inhibitor 99.97%
    ZED-1227 is a specific and orally active 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).
    Vilagletistat
  • HY-W020050
    Cystamine dihydrochloride
    		Inhibitor 99.92%
    Cystamine (dihydrochloride) is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD) .
    Cystamine dihydrochloride
  • HY-P99512
    Zampilimab
    		Inhibitor ≥99.0%
    Zampilimab (UCB-7858) is a monoclonal antibody against transglutaminase 2 (TG2). Zampilimab inhibits TG2 crosslinking transamidation activity with an IC50 of 0.25 nM and a Kd of <50 pM. Zampilimab improves renal fibrosis.
    Zampilimab
  • HY-117678
    TG-2-IN-1
    		Inhibitor 98.0%
    TG-2-IN-1 (Compound D003) is a transglutaminase-2 (TGM-2) inhibitor. TG-2-IN-1 can be used for the research of myopia.
    TG-2-IN-1
  • HY-121167
    L-Albizziin
    		Inhibitor 98.0%
    L-albizziin, as a sulfhydryl group reagent, is a glutamase inhibitor. L-albizziin can be used for the research of cancer.
    L-Albizziin
  • HY-123290
    KCC009
    		Inhibitor 98.06%
    KCC009, a transglutaminase 2 (TG2) inhibitor, induces p53-independent radiosensitization.
    KCC009
  • HY-129126
    NC9
    		Inhibitor 99.98%
    NC9 (Cbz-Lys(Acr)-PEG2-dansyl) is an irreversible transglutaminase (TG) inhibitor. NC9 inhibits osteoblast differentiation and mineralization. NC9 destabilizes microtubules. NC9 can be used for the research of osteoblast differentiation.
    NC9
Cat. No. Product Name / Synonyms Application Reactivity