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
  • 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.
  • HY-12683
    BPTES
    		Inhibitor 98.09%
    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 99.92%
    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.
  • HY-122218
    JHU-083
    		Antagonist ≥98.0%
    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.
  • HY-12682
    Glutaminase C-IN-1
    		Inhibitor 99.88%
    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-145933
    BJJF078
    		Inhibitor
    BJJF078 is an aminopiperidine derivative. BJJF078 is a potent inhibitor of recombinant human and mouse Transglutaminase enzyme (TG2) activity, IC50 values of 41 and 54 nM, respectively. BJJF078 also inhibits the close related enzyme TG1, with an IC50 of 0.16 μM. BJJF078 can be used for Multiple sclerosis (MS) research.
  • HY-102073
    TG53
    		Inhibitor
    TG53 is a potent inhibitor of tissue transglutaminase (TG2) and fibronectin (FN) protein-protein interaction. TG53 inhibits formation of a complex with integrin β1 and activation of FAK and c-Src during SKOV3 cell attachment onto FN. TG53 can be used for ovarian cancer research.
  • HY-155138
    GLS1 Inhibitor-7
    		Inhibitor
    GLS1 Inhibitor-7 (compound 4d) is a GLS1 inhibitor (IC50=46.7 μM), with potential anti-cancer, anti-aging and anti-obesity properties.
  • HY-19359
    ZED-1227
    		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).
  • HY-12337
    GK921
    		Inhibitor 99.93%
    GK921 is a transglutaminase 2 (TGase) inhibitor with an IC50 of 7.71 μM for human recombinant TGase 2.
  • HY-103671
    IPN60090
    		Inhibitor 99.47%
    IPN-60090 is an orally active and highly selective inhibitor of glutaminase 1 (GLS1; IC50=31 nM), with no activity observed against GLS-2. IPN-60090 exhibits excellent physicochemical and pharmacokinetic properties in vivo. IPN-60090 can be used for solid tumors research, such as lung and ovarian cancers.
  • HY-114334
    Glutaminase-IN-1
    		Inhibitor 98.65%
    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-124476
    Cystamine
    		Inhibitor 99.79%
    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) .
  • HY-79583
    Glutaminase-IN-3
    		Inhibitor 98.47%
    Glutaminase-IN-3 (compound 657) is a potent glutaminase inhibitor with an IC50 of 0.24 μM for Glutaminase 1 (GLS1). Glutaminase-IN-3 is extracted from patent WO2014089048A1, compound 657.
  • 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.
  • 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.
  • HY-W020050
    Cystamine (dihydrochloride）
    		Inhibitor ≥98.0%
    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) .
  • 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.
  • HY-103671A
    IPN60090 dihydrochloride
    		Inhibitor 99.05%
    IPN-60090 dihydrochloride is an orally active and highly selective inhibitor of glutaminase 1 (GLS1; IC50=31 nM), with no activity observed against GLS-2. IPN-60090 dihydrochloride exhibits excellent physicochemical and pharmacokinetic properties in vivo. IPN-60090 dihydrochloride can be used for solid tumors research, such as lung and ovarian cancers.
  • HY-123290
    KCC009
    		Inhibitor 98.98%
    KCC009, a transglutaminase 2 (TG2) inhibitor, induces p53-independent radiosensitization.
Cat. No. Product Name / Synonyms Application Reactivity