GPNA hydrochloride Amino acid transporter inhibitor

Cat.No.S6670

GPNA hydrochloride (L-γ-glutamyl-p-nitroanilide hydrochloride) is a substrate of γ-glutamyltransferase (GGT) and an inhibitor of the glutamine transporter ASCT2 with an IC50 of ~250 μM in A549 cells. It also inhibits Na+-dependent carriers SNAT1, -2, -4, -5 and Na+-independent leucine transporters LAT1/2. It can be widely used in research on pancreatic cancer, breast cancer, glioblastoma multiforme, acute myelogenous leukemia, and non-small-cell lung cancer.
GPNA hydrochloride Amino acid transporter inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 303.7

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 303.7 Formula

C11H14ClN3O5

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 67953-08-6 Download SDF Storage of Stock Solutions

Solubility

In vitro
Batch:

DMSO : 5 mg/mL (16.46 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

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Mechanism of Action

Targets/IC50/Ki
ASCT2 [1]
(Cell-free assay)
55 μM(Ki)
In vitro

GPNA leads to a significant decrease in endometrial cancer cell growth and spheroid cross-sectional area.[1]

In vivo

EGFRAS-GPNA (EGFRAS-specific GPNA oligomers) is taken-up by several tissues including the xenograft tumor. Systemic administration of EGFRAS-GPNA induces antitumor effects in HNSCC xenografts, with similar efficacies as the FDA-approved EGFR inhibitors: cetuximab and erlotinib. EGFRAS-GPNA effectively againsts the constitutively active EGFR vIII mutant implicated in cetuximab resistance.

References

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