| S8620 |
6-Diazo-5-oxo-L-norleucine (Diazooxonorleucine)
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6-Diazo-5-oxo-L-norleucine (Diazooxonorleucine, L-6-Diazo-5-oxonorleucine, DON), an antibiotic isolated from Streptomyces, is a glutaminase antagonist with IC50 of ~1 mM for cKGA (kidney-type glutaminase). 6-Diazo-5-oxo-L-norleucine exhibits analgesic, antibacterial, antiviral and anticancer properties.
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bioRxiv, 2025, 2025.07.14.664742
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Int J Mol Sci, 2024, 25(18)10183
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iScience, 2023, 26(10):107790
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| S8891 |
JHU-083
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JHU-083 (Ethyl 2-(2-Amino-4-methylpentanamido)-DON) is a novel prodrug of DON. This compound selectively blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress.Solutions are unstable and should be fresh-prepared.
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Cell Rep, 2025, 44(5):115596
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Cell Reports, 2025, 115596
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Molecular Cancer, 2023, 85
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| S8892 |
JHU395
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JHU395 is a novel orally bioavailable GA (glutamine antagonists) prodrug designed to circulate inert in plasma, but permeate and release active GA within target tissues. This compound delivers active GA to malignant peripheral nerve sheath tumor (MPNST), and significantly inhibits tumor growth without observed toxicity.
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| E1203 |
Sirpiglenastat (DRP-104)
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Sirpiglenastat (DRP-104) is a broad acting glutamine antagonist. It has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response with immunomodulatory and antineoplastic activities.
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