| Identification | Back Directory | [Name]
R162 | [CAS]
64302-87-0 | [Synonyms]
R162, >98%
R162;R-162;R 162
2-Allyl-1-hydroxy-9,10-anthraquinone
9,10-Anthracenedione, 1-hydroxy-2-(2-propen-1-yl)- | [Molecular Formula]
C17H12O3 | [MDL Number]
MFCD00666806 | [MOL File]
64302-87-0.mol | [Molecular Weight]
264.28 |
| Chemical Properties | Back Directory | [Melting point ]
120-120.5 °C(Solv: acetone (67-64-1)) | [Boiling point ]
459.0±34.0 °C(Predicted) | [density ]
1.308±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (up to 10 mg/ml or in Ethanol (up to 5 mg/ml) | [form ]
solid | [pka]
7.43±0.20(Predicted) | [color ]
Orange | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [Description]
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. | [Uses]
R162 is a glutamate dehydrogenase 1 inhibitor for the treatment of cancer. A useful bioactive chemical compound. | [Definition]
ChEBI: 2-allyl-1-hydroxy-9,10-anthraquinone is a monohydroxyanthraquinone that is 9,10-anthraquinone in which the hydrogens at positions 1 and 2 are replaced by a hydroxy and an allyl group, respectively. It has a role as an EC 1.4.1.3 {glutamate dehydrogenase [NAD(P)(+)]} inhibitor. | [in vivo]
R162 (30 mg/kg/day, i.p.) does not result in a significant histopathological change between the vehicle-treated and R162-treated groups, nor alters complete blood counts, or hematopoietic properties in xenograft tumor mouse models. R162 (20 mg/kg/day) results in significantly decreased tumor growth and masses in mice compared with control mice and effectively inhibits GDH1 activity in resected tumors from xenograft nude mice[1]. | [References]
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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