Home Proteases Glutaminase antagonist 6-Diazo-5-oxo-L-norleucine For research use only.

6-Diazo-5-oxo-L-norleucine

Synonyms: Diazooxonorleucine, 6-Diazo-5-oxo-L-nor-Leucine, L-6-Diazo-5-oxonorleucine, DON

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.

6-Diazo-5-oxo-L-norleucine Chemical Structure

6-Diazo-5-oxo-L-norleucine Chemical Structure

CAS No. 157-03-9

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6-Diazo-5-oxo-L-norleucine Related Products

Biological Activity

Description 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.
Targets
cKGA [1]
(Cell-free assay)
1 mM
In vitro
In vitro

6-Diazo-5-oxo-L-norleucine appears to be positive in the in vitro chromosome aberration assay that it demonstrates dose dependent statistically positive increase in structural aberrations at 4 and 20 hour exposure without S9 and also at 4 hour exposure with S9.[2]
Cell Research Cell lines Chinese hamster ovary (CHO) cells
Concentrations 0.1712 μg/mL to 1712 μg/mL
Incubation Time 4 h, 20 h
Method

CHO cells are exposed to vehicle alone and to nine dose levels of test article, ranging from 0.1712 to 1712 μg/mL in the absence or presence of an S9 reaction mixture.
In Vivo
In vivo

6-Diazo-5-oxo-L-norleucine is evaluated for its in vivo clastogenic activity by detecting micronuclei in polychromatic erythrocyte (PCE) cells in bone marrow collected from the male mice dosed intravenously with 500, 100, 10, 1 and 0.1 mg/kg at 24 and 48 hour post dose. The in vivo micronucleus assay reveals a statistically positive response for micronucleus formation at 500, 100 and 10 mg/kg at 24 and 48 hour post dose.[2]
Animal Research Animal Models 6-week-old male ICR mice
Dosages 500 mg/kg, 100 mg/kg, 10 mg/kg, 1 mg/kg, 0.1 mg/kg
Administration IV
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06373094 Not yet recruiting
Alzheimer Disease
Shanghai Synergy Pharmaceutical Sciences Co. Ltd.|Zhejiang Huahai Pharmaceutical Co. Ltd.
 June 1 2024 Phase 1
NCT06261541 Recruiting
Multiple Sclerosis
ABLE Human Motion S.L.|Fundación Esclerosis Múltiple Madrid (FEMM)
 April 8 2024 Not Applicable
NCT06167954 Recruiting
Cerebral Palsy|Acquired Brain Injury|Spinal Muscular Atrophy
MarsiBionics|Hospital Infantil Universitario Niño Jesús Madrid Spain|Hospital Universitario La Paz|Hospital Universitario 12 de Octubre|Hospital General Universitario Gregorio Marañon
 December 4 2023 Not Applicable
NCT05914818 Completed
Cerebral Palsy|Acquired Brain Injury|Neuromuscular Diseases in Children
MarsiBionics|National Research Council Spain|Hospital Infantil Universitario Niño Jesús Madrid Spain|Hospital Universitario La Paz|Hospital Universitario 12 de Octubre|Hospital General Universitario Gregorio Marañon
 June 23 2023 Not Applicable

Chemical Information & Solubility

Molecular Weight 171.15 Formula

C6H9N3O3
CAS No. 157-03-9 SDF --
Smiles C(CC(=O)C=[N+]=[N-])C(C(=O)O)N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

Water : 34 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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In vivo
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