纯度:98% by TLC,;NMR (Conforms)
分子式:C17H12O3
分子量:264.28
溶剂:DMSO (10 mg/ml) Ethanol (5 mg/ml)
性状:Orange solid
存储:-20°C
Activity (short version):Glutamate Dehydrogenase 1 inhibitor
Function / Pharmacology: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 lead 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 us a useful tool for proof of principal studies.