GPNA hydrochloride

Names

[ Name ]:
GPNA hydrochloride

[Synonym ]:
L-GLUTAMIC ACID γ-(P-NITROANILIDE) HYDROCHLORIDE

Biological Activity

[Description]:

GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor. GPNA hydrochloride also inhibit Na+-dependent carriers, such as SNAT family (SNAT1/2/4/5), and the Na+-independent leucine transporters LAT1/2. GPNA reversibly induces apoptosis in A549 cells[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

[Target]

ASCT2[1]

[In Vitro]

GPNA (10-1000 μM; 48 hours) induces a dose-dependent decrease of cell viability in A549 cells[1]. Cell Viability Assay[1] Cell Line: A549 cells Concentration: 10, 100, 250, 500 , and 1000 μM Incubation Time: 48 hours Result: Induced a dose-dependent decrease of cell viability, with an IC50 roughly corresponding to ~250 μM.

[References]

[1]. Corti A, et al. γ-Glutamyltransferase enzyme activity of cancer cells modulates L-γ-glutamyl-p-nitroanilide (GPNA) cytotoxicity. Sci Rep. 2019 Jan 29;9(1):891.

Chemical & Physical Properties

[ Boiling Point ]:
590.6ºC at 760 mmHg

[ Molecular Formula ]:
C₁₁H₁₄ClN₃O₅

[ Molecular Weight ]:
303.69900

[ Flash Point ]:
311ºC

[ Exact Mass ]:
303.06200

[ PSA ]:
138.24000

[ LogP ]:
2.82390

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

Articles

Donor substrate specificity of bovine kidney gamma-glutamyltransferase

Chem. Biol. Interact. 203(2) , 480-5, (2013)

Highlights • Five aromatic or polycyclic aromatic glutathione conjugates were synthesized. • Enzyme kinetic studies were performed for each conjugate as a γ-glutamyltransferase (GGT) donor substrate. ...

Cross-talk between ER and HER2 regulates c-MYC-mediated glutamine metabolism in aromatase inhibitor resistant breast cancer cells.

J. Steroid Biochem. Mol. Biol. 149 , 118-27, (2015)

Resistance to endocrine therapies in hormone receptor (HR)-positive breast cancer is a significant clinical problem for a considerable number of patients. The oncogenic transcription factor c-MYC (her...

Rapid purification and characterization of γ-glutamyl-transpeptidase from shiitake mushroom (Lentinus edodes).

J. Food Sci. 77(6) , C640-5, (2012)

γ-Glutamyl-transpeptidase (GGT) is one of the important enzymes in the pathway of odor formation in shiitake mushroom (Lentinus edodes). Rapid purification and characterization of GGT from shiitake mu...