| 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 behaviours 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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iScience, 2023, 26(10):107790
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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 tumour (MPNST), and significantly inhibits tumour 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 tumour metabolism and simultaneously inducing a potent anti-tumour immune response with immunomodulatory and antineoplastic activities.
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