64302-87-0

64302-87-0 structure

Name: R162
Chemical Name: R162
CAS Number: 64302-87-0
Molecular Formula: C₁₇H₁₂O₃
Molecular Weight: 264.275
Catalog: Research Areas Cancer
Create Date: 2018-03-08 17:51:34
Modify Date: 2024-01-03 17:34:41
R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1), with anti-cancer properties.

Name	R162
Synonyms	9,10-Anthracenedione, 1-hydroxy-2-(2-propen-1-yl)- 2-Allyl-1-hydroxy-9,10-anthraquinone

Description	R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1), with anti-cancer properties.
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Cancer
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].
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 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.