R162 |
| カタログ番号GC32750 |
R162 は、グルタミン酸デヒドロゲナーゼ 1 (GDH1/GLUD1) の強力な阻害剤であり、抗がん特性があります。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 64302-87-0
Sample solution is provided at 25 µL, 10mM.
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R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1), with anti-cancer properties.
Inhibition of GDH1 activity by R162 treatment results in decreased intracellular fumarate levels, attenuated GPx activity, increased ROS levels, and reduced cell proliferation in H1299 and MDA-MB231 cells, which can be significantly rescued by methyl-α-KG treatment as well as by antioxidant NAC. R162 inhibits cell proliferation and tumor growth potential of human cancer cells[1].
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].
[1]. Jin L, et al. Glutamate dehydrogenase 1 signals through antioxidant glutathione peroxidase 1 to regulate redox homeostasis and tumor growth. Cancer Cell. 2015 Feb 9;27(2):257-70.
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