GPNA hydrochloride

Catalog No.S6670 Batch:S667002

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Technical Data

Formula

C11H14ClN3O5
Molecular Weight 303.7 CAS No. 67953-08-6
Solubility (25°C)* In vitro DMSO 5 mg/mL (16.46 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description 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.
Targets
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.

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    Endometrial cancer cell line

  • Concentrations

    1 mM

  • Incubation Time

    24 h

  • Method

    Cells (1–2 × 105) are cultured for 24 h followed by treatment where stated with vehicle or 1 mm GPNA for 24 h. And then staining for flow cytometric analysis is performed. MTT assays are conducted using 100–250 cells per well in a 96-well plate. Fresh media with vehicle or 1 mm GPNA are applied every two days.

Selleck's GPNA hydrochloride has been cited by 5 publications

Lipophagy-mediated cholesterol synthesis inhibition is required for the survival of hepatocellular carcinoma under glutamine deprivation [ Redox Biol, 2023, 63:102732] PubMed: 37150151
Inhibition of SND1 overcomes chemoresistance in bladder cancer cells by promoting ferroptosis [ Oncol Rep, 2023, 49(1)16] PubMed: 36453257
Neddylation inhibition induces glutamine uptake and metabolism by targeting CRL3SPOP E3 ligase in cancer cells [ Nat Commun, 2022, 13(1):3034] PubMed: 35641493
Antagonizing Glutamine Bioavailability Promotes Radiation Sensitivity in Prostate Cancer [ Cancers (Basel), 2022, 14(10)2491] PubMed: 35626095
Evaluation of Glutaminolysis in T Cells [ Curr Protoc, 2022, 2(9):e540] PubMed: 36111948

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.