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JHU-083 Glutaminase antagonist

Name: JHU-083
Brand: Selleck Chemicals
SKU: S8891
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S8891

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.

Chemical Structure

Molecular Weight: 312.36

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Quality Control

Batch: Purity: 99.85%

99.85

Related Targets	HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease DPP Tyrosinase HIV Protease
Other Glutaminase Products	Telaglenastat (CB-839) Sirpiglenastat (DRP-104) BPTES GK921 Zampilimab (Anti-TGM2 / Transglutaminase 2) TGM2 Antibody [K23K16] LDN-27219 JHU395 6-Diazo-5-oxo-L-norleucine (Diazooxonorleucine) UPGL00004

Solubility

In vitro
Batch:

DMSO : 62 mg/mL (198.48 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 15 mg/mL

Water : 8 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.100mg/ml (9.92mM)	Taking the 1 mL working solution as an example, add 50 μL 62 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	312.36	Formula	C₁₄H₂₄N₄O₄	Storage (From the date of receipt)	3 years -20°C(in the dark) powder
CAS No.	1998725-11-3	--		Storage of Stock Solutions	Solutions are unstable. Prepare fresh or purchase small, pre-packaged sizes. Repackage upon receipt.
Synonyms	Ethyl 2-(2-Amino-4-methylpentanamido)-DON			Smiles	CCOC(=O)C(CCC(=O)C=[N+]=[N-])NC(=O)C(CC(C)C)N

Mechanism of Action

Targets/IC₅₀/Ki	Glutaminase
In vitro	This compound selectively inhibits T-cell proliferation and decreases T-cell activation, with no eﬀect on DCs.
In vivo	In vivo, orally administered JHU-083 significantly decreases the experimental autoimmune encephalomyelitis(EAE) severity in both prevention and treatment paradigms and reverses EAE-induced cognitive impairment.
References	[1] https://pubmed.ncbi.nlm.nih.gov/30127344/ [2] https://pubmed.ncbi.nlm.nih.gov/31467038/

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