968
Chemical Name: 5-[3-Bromo-4-(dimethylamino)phenyl]-2,3,5,6-tetrahydro-2,2-dimethylbenzo[a]phenanthridin-4(1H)-one
Purity: ≥99%
Biological Activity
968 is an allosteric inhibitor of glutaminase. Blocks Rho-GTPase-dependent transformation of fibroblasts. Suppresses breast cancer cell growth and invasive activity in vitro. Also inhibits P-493 B lymphoma cell growth and reduces tumor size of P-493 cell xenografts in mice.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Targeting mitochondrial glutaminase activity inhibits oncogenic transformation.
Wang et al.
Cancer Cell, 2010;18:207 -
Mechanism by which a recently discovered allosteric inhibitor blocks glutamine metabolism in transformed cells.
Stalnecker et al.
Proc.Natl.Acad.Sci.U.S.A., 2015;112:394 -
Cancer metabolism: is glutamine sweeter than glucose?
Lu et al.
Cancer Cell, 2010;18:199
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