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.
|Storage||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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 475.42. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.1 mL||10.52 mL||21.03 mL|
|5 mM||0.42 mL||2.1 mL||4.21 mL|
|10 mM||0.21 mL||1.05 mL||2.1 mL|
|50 mM||0.04 mL||0.21 mL||0.42 mL|
References are publications that support the products' biological activity.
Wang et al (2010) Targeting mitochondrial glutaminase activity inhibits oncogenic transformation. Cancer Cell 18 207 PMID: 20832749
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
If you know of a relevant reference for 968, please let us know.
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Keywords: 968, supplier, Hydrolases, allosteric, inhibitors, inhibits, glutaminase, oncogene, transformation, gls1, Glutaminase, Glutaminase, Tocris Bioscience
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Cancer Metabolism Poster
Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the main targets for cancer metabolism researchers. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways. These distinct metabolic circuits could provide viable cancer therapeutic targets.