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JHU395

Chemical Structure : JHU395

CAS No.: 2079938-92-2

JHU395 (JHU-395)

Catalog No.: PC-38668Not For Human Use, Lab Use Only.

JHU395 is orally-bioavailable glutamine antagonist prodrug, shows antitumor activity in malignant peripheral nerve sheath tumor (MPNST, sNF96.2 cell growth IC50=4.6 uM).

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Biological Activity

JHU395 is orally-bioavailable glutamine antagonist prodrug, shows antitumor activity in malignant peripheral nerve sheath tumor (MPNST, sNF96.2 cell growth IC50=4.6 uM).
JHU395 exhibits increased metabolic stability in swine and human plasma, favorable conversion in brain homogenate, and substantially improved CNS delivery in vivo in swine, compare with 6-diazo-5-oxo-L-norleucine (DON).
JHU395 attenuates glutamate synthesis in HIV-infected microglia/macrophages, offering therapeutic potential for HIV-associated neurocognitive disorders (HAND).
JHU395 also decreased growth and increased apoptosis in multiple human high-MYC medulloblastoma cell lines at lower concentrations than DON.

Physicochemical Properties

M.Wt 447.488
Formula C22H29N3O7
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-Diazo-N-[[(2,2-dimethyl-1-oxopropoxy)phenylmethoxy]carbonyl]-5-oxo-L-norleucine 1-methylethyl ester

References

1. Nedelcovych MT, et al. J Med Chem. 2017;60:7186–98.

2. Lemberg KM, et al. Mol Cancer Ther. 2020 Feb;19(2):397-408.

3. Khoa Pham, et al. J Neuropathol Exp Neurol. 2021 Mar 22;80(4):336-344.

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