For research use only. Not for therapeutic Use.
JHU-083, a proagent 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].
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].
| Catalog Number | I018738 |
| CAS Number | 1998725-11-3 |
| Synonyms | ethyl (2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-6-diazo-5-oxohexanoate |
| Molecular Formula | C14H24N4O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C14H24N4O4/c1-4-22-14(21)12(6-5-10(19)8-17-16)18-13(20)11(15)7-9(2)3/h8-9,11-12H,4-7,15H2,1-3H3,(H,18,20)/t11-,12-/m0/s1 |
| InChIKey | YZRCHOFKIPHQBW-RYUDHWBXSA-N |
| SMILES | CCOC(=O)C(CCC(=O)C=[N+]=[N-])NC(=O)C(CC(C)C)N |
| 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. |
