Cas No.: | 64302-87-0 |
Chemical Name: | R162,R-162,R 162 |
Synonyms: | R162,R-162,R 162 |
SMILES: | O=C(C1=C2C=CC=C1)C3=CC=C(CC=C)C(O)=C3C2=O |
Formula: | C17H12O3 |
M.Wt: | 264.28 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1), with anti-cancer properties. |
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]. |
In Vitro: | 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]. |