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-79583
    Glutaminase-IN-3
    		Inhibitor 99.88%
    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.
    Glutaminase-IN-3
  • 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.
    UPGL00004
  • HY-145933
    BJJF078
    		Inhibitor 99.34%
    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.
    BJJF078
  • HY-160132
    TG-2-IN-4
    		Inhibitor 99.62%
    TG-2-IN-4 (compound 8) is a transglutaminase 2 (TG2) inhibitor with an IC50 <0.5 mM. TG-2-IN-4 can be used for the research of inflammatory disorder.
    TG-2-IN-4
  • HY-103671A
    IPN60090 dihydrochloride
    		Inhibitor 99.68%
    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.
    IPN60090 dihydrochloride
  • HY-155102
    PROTAC TG2 degrader-2
    		Degrader 99.15%
    PROTAC TG2 degrader-2 (compound 7) is a selective, competitive degrader targeting Transglutaminase 2 (TG2), with Kd > 100 μM. PROTAC TG2 degrader-2 inhibits the cell migration and decreases the level of TG2 in ovarian cancer cells. PROTAC TG2 degrader-2 can be used for ovarian cancer study.
    PROTAC TG2 degrader-2
  • HY-W006187
    2-Amino-2-(p-tolyl)acetic acid
    		Inhibitor
    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
  • HY-144666
    GLS-1-IN-1
    		Inhibitor 99.64%
    GLS-1-IN-1 (compound 1d) is a GLS-1 inhibitor. GLS-1-IN-1 shows inhibitory effect against Hep G2, MCF 7, and MCF 10A cells.
    GLS-1-IN-1
  • HY-136704
    GLS1 Inhibitor-1
    		Inhibitor 98.5%
    GLS1 Inhibitor-1 (Compound 27) is an orally active inhibitor for glutaminase 1 (GLS1) with an IC50 of 0.021 μM. GLS1 Inhibitor-1 inhibits the proliferation of PC-3 with an IC50 of 0.3 nM. GLS1 Inhibitor-1 exhibits antitumor efficacy against NCI-H1703 with GI50 of 0.011 μM. GLS1 Inhibitor-1 exhibits moderate pharmacokinetic characteristics.
    GLS1 Inhibitor-1
  • HY-122709
    hTG2 inhibitor VA4
    		Inhibitor
    hTG2 inhibitor VA4 (compound VA4) is an irreversible Type 2 transglutaminase (TG2) inhibitor. hTG2 inhibitor VA4 reacts exclusively at the TG2 transamidase site, inhibits both transamidase and GTP-binding activities.
    hTG2 inhibitor VA4
  • HY-12248A
    Telaglenastat hydrochloride
    		Inhibitor
    Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride 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 hydrochloride inudces autophagy and has antitumor activity.
    Telaglenastat hydrochloride
  • HY-151434
    GLS1 Inhibitor-6
    		Inhibitor
    GLS1 Inhibitor-6 (Compound 24y) is an orally active, potent and selective glutaminase 1 (GLS1) inhibitor (IC50=68 nM), shows 220-fold selectivity for GLS2. GLS1 Inhibitor-6 shows good anti-tumor activity, antitumor cell proliferation activity and induces apoptosis.
    GLS1 Inhibitor-6
  • HY-147718
    α-Glucosidase-IN-5
    		Inhibitor
    α-Glucosidase-IN-5 (compound 8) is a potent α-glucosidase inhibitor with an IC50 of 57.9 µM. α-Glucosidase-IN-5 has the potential for the research of diabetes mellitus.
    α-Glucosidase-IN-5
  • 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.
    TG53
  • 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.
    GLS1 Inhibitor-7
  • HY-146616
    GLS1 Inhibitor-3
    		Inhibitor
    GLS1 Inhibitor-3 (compound C147) is a potent GLS1 inhibitor with an IC50 of 27.98 nM. GLS1 Inhibitor-3 shows antiproliferative activity.
    GLS1 Inhibitor-3
  • HY-125958
    AA9
    		Inhibitor
    AA9 is a potent Transglutaminase 2 (TG2) inhibitor. AA9 strongly impacts HIF-mediated hypoxia in MDA-MB-231 cells.
    AA9
  • HY-146658
    Glutaminase-IN-4
    		Inhibitor
    Glutaminase-IN-4 (compound 2a) is a glutaminase (GLS) inhibitor with an IC50 of 2.3 μM.
    Glutaminase-IN-4
  • HY-100446
    NTU281
    		Inhibitor
    NTU281 is a potent transglutaminase-2 inhibitor. NTU281 can reduce the increases in serum creatinine and albuminuria in diabetic rats. NTU281 can also reduce glomerular collagen I accumulation, Hic-5 and α-SMA expression, and apoptosis. NTU281 can be used for researching glomerulosclerosis caused by diabetes.
    NTU281
  • HY-158378
    Trivalent hydroxyarsinothricn
    		Inhibitor
    Trivalent hydroxyarsinothricn (R-AST-OH) is a covalent and irreversible kidney-type glutaminase (KGA) inhibitor. Trivalent hydroxyarsinothricn binds to the glutamine binding site and forms a covalent bond with an active site cysteine residue. Trivalent hydroxyarsinothricn selectively kills triple-negative breast cancer (TNBC) cells and is not cytotoxic to the control cell line. KGA is the enzyme that controls glutamine metabolism and is correlated with tumor malignancy.
    Trivalent hydroxyarsinothricn
Cat. No. Product Name / Synonyms Application Reactivity