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R162 | Glutamate dehydrogenase 1 inhibitor

R162 (64302-87-0) is a selective inhibitor of glutamate dehydrogenase 1 (GDH1), a commonly upregulated enzyme in human cancers (Ki = 28.6 µM).  It does not inhibit the activity of other NADPH enzymes such as 6-phosphogluconate dehydrogenase and fumarate hydratase. R162 treatment leads to decreased fumarate levels, lower glutathione peroxidase activity, increased ROS levels and reduced cell proliferation in H1299 and MDA-MB231 cells.  R162 sensitizes LKB-1 deficient tumor cells to anoikis induction.  R162 treatment (at 20 mg/kg/day) significantly attenuates metastatic potential in a xenograft mouse model.2  GDH1 is a promising antimetastasis target and R162 is a useful tool for proof of principal studies.

References/Citations

1) Jin et al. (2015), Glutamate Dehydrogenase 1 Signals through Antioxidant Glutathione Peroxidase 1 to Regulate Redox Homeostasis and Tumor Growth; Cancer Cell, 27 257
2) Jin et al. (2018) The PLAG1-GDH1 Axis Promotes Anokis Resistance and Tumor Metastasis through CamKK2-AMPK Signaling in LKB1-Deficient Lung Cancer; Mol. Cell, 69 1

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Catalog#  10-4603-0010

$50.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
64302-87-0
Catalog Number:
10-4603
Activity:
Glutamate Dehydrogenase 1 inhibitor
Chemical Name:
1-Hydroxy-2-(2-propen-1-yl)-9,10-anthracenedione
Alternate Names:
Purpurin analog
Molecular Weight:
264.28
Molecular Formula:
C17H12O3
Solubility:
Soluble in DMSO (up to 10 mg/ml or in Ethanol (up to 5 mg/ml)
Physical Properties:
Orange solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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