| Bioactivity | JHU-083, a prodrug 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[1][2]. |
| In Vivo | JHU-083 (1.82 mg/kg; PO; every other day for 12 days) ameliorates social avoidance behavior and anhedonia-like behavior induced by CSDS[1]. JHU-083 (1.82 mg/kg, PO) attenuates CSDS-induced increase in glutaminase activity in CD11b+ cells in the prefrontal cortex and hippocampus, but not in the cerebellum. JHU-083 treatment suppresses the CSDS-induced upregulation of IL-1β and TNF-α expression[1]. Animal Model: |
| Name | JHU-083 |
| CAS | 1998725-11-3 |
| Formula | C14H24N4O4 |
| Molar Mass | 312.36 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Zhu X, et al. JHU-083 selectively blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress. Neuropsychopharmacology. 2019 Mar;44(4):683-694. [2]. Riggle BA, et al. MRI demonstrates glutamine antagonist-mediated reversal of cerebral malaria pathology in mice. Proc Natl Acad Sci U S A. 2018 Dec 18;115(51):E12024-E12033. |