Cat. No. 5460

968 C27H27BrN2O [311795-38-7]

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Chemical Name: 5-[3-Bromo-4-(dimethylamino)phenyl]-2,3,5,6-tetrahydro-2,2-dimethylbenzo[a]phenanthridin-4(1H)-one

Biological Activity

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

Soluble to 20 mM in DMSO
>99 %
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

Stalnecker et al (2015) Mechanism by which a recently discovered allosteric inhibitor blocks glutamine metabolism in transformed cells. Proc.Natl.Acad.Sci.U.S.A. 112 394. PMID: 25548170.

Lu et al (2010) Cancer metabolism: is glutamine sweeter than glucose? Cancer Cell 18 199. PMID: 20832746.

Wang et al (2010) Targeting mitochondrial glutaminase activity inhibits oncogenic transformation. Cancer Cell 18 207. PMID: 20832749.

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Keywords: 968, supplier, Hydrolases, allosteric, inhibitors, inhibits, glutaminase, oncogene, transformation, gls1, Tocris Bioscience, Glutaminase Inhibitor products

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