| Bioactivity | R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1/GLUD1), with anti-cancer properties. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| 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]. | ||||||||||||
| Name | R162 | ||||||||||||
| CAS | 64302-87-0 | ||||||||||||
| Formula | C17H12O3 | ||||||||||||
| Molar Mass | 264.28 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |