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Cat.No. 5460 - 968 | C27H27BrN2O | CAS No. 311795-38-7
Description: Allosteric inhibitor of glutaminase
Chemical Name: 5-[3-Bromo-4-(dimethylamino)phenyl]-2,3,5,6-tetrahydro-2,2-dimethylbenzo[a]phenanthridin-4(1H)-one
Purity: ≥99% (HPLC)
Literature (2)

Biological Activity for 968

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 for 968

M. Wt 475.42
Formula C27H27BrN2O
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 311795-38-7
PubChem ID 3099980
Smiles BrC1=CC(C(C5=C4CC(C)(C)CC5=O)NC3=C4C2=CC=CC=C2C=C3)=CC=C1N(C)C

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.

Solubility Data for 968

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 9.51 20

Preparing Stock Solutions for 968

The following data is based on the product molecular weight 475.42. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 10.52 mL 52.59 mL 105.17 mL
1 mM 2.1 mL 10.52 mL 21.03 mL
2 mM 1.05 mL 5.26 mL 10.52 mL
10 mM 0.21 mL 1.05 mL 2.1 mL

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References for 968

References are publications that support the biological activity of the product.

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, 968 supplier, Hydrolases, allosteric, inhibitors, inhibits, glutaminase, oncogene, transformation, gls1, Glutaminase, 5460, Tocris Bioscience

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