Glutaminase is the initial enzyme in glutamine metabolism, which catalyzes the hydrolysis of glutamine to glutamate in cells.The metabolism, growth, and proliferation of cancer cells are significantly influenced by glutaminase. GLS1 (or GLS) and GLS2, two paralogous GLS genes, are present in mammalian cells. Kidney glutaminase (KGA) and glutaminase C (GAC) are two alternatively spliced isozymes that are encoded by the gene GLS1. Additionally, liver glutaminase (LGA) and glutaminase B are encoded by GLS2.
The oncogene MYC has the ability to increase the expression of GLS1, which is present in all tissues and is ubiquitously expressed. Hepatocellular carcinoma (HCC) is one type of cancer where GLS1 is frequently activated and/or overexpressed. Due to its glutaminase activity and function in promoting glutamine metabolism, GLS1 has been shown to promote tumorigenesis in a variety of cancer types, including HCC. A crucial enzyme in several different cancer types has been identified as GLS. In vitro and in vivo tumor cell growth has also been linked to increased GLS2 enzymatic activity.When N-Myc activates GLS2, MYCN-amplified neuroblastoma cells are more likely to convert glutamine to glutamate. Glutaminolysis is severely inhibited when GLS2 function is lost, and both in vitro and in vivo cell proliferation and survival are significantly reduced. However, there is disagreement regarding GLS2's function as a tumor suppressor. Through p53 or p63, GLS2-independent enzymatic activity is increased and functions as a tumor suppressor.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V1897 | BPTES | 314045-39-1 | BPTES is a potent and selective allosteric Glutaminase GLS1 (KGA) inhibitor with IC50 of 0.16 μM. |
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V9211 | Diazooxonorleucine | 157-03-9 | 6-Diazo-5-oxo-L-nor-Leucine (L-6-Diazo-5-oxonorleucine; DON) is a glutamine antagonist that irreversibly inhibits the breakdown of glutamine. |
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V4158 | GK921 | 1025015-40-0 | GK921 is a novel and potent inhibitor of transglutaminase 2 (TGase) with an IC50 of 7.71 μM for human recombinant TGase 2. |
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V21635 | GLS-IN-968 | 311795-38-7 | GLS-IN-968 is an allosteric inhibitor of glutaminase (GLS). |
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V40795 | IPN-60090 ( IACS-6274) | 1853164-83-6 | IPN-60090( IACS-6274; IPN60090) is a novel, potent, orally bioavailable and specific inhibitor of GLS1 (the kidney-type glutaminase), which is an important enzyme for metabolic energy production. |
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V1876 | STF-31 | 724741-75-7 | STF-31 is anovel potent and selective glucose transporter (GLUT1) inhibitor with IC50 of 1 μM. |
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V1899 | Telaglenastat (CB-839) | 1439399-58-2 | Telaglenastat (formerly known as CB-839) is a novel,investigational, potent, selective, and orally bioavailablesmall molecule glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. |
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V4103 | UPGL00004 | 1890169-95-5 | UPGL00004 (UPGL-00004) is a novel, potent and allosteric inhibitor ofglutaminase C (GAC, kidney glutaminase isoform C) with anticancer activity. |
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