Biochem/physiol Actions

Reversible: yes

Primary Targetmitochondrial glutaminase

Cell permeable: yes

General description

A cell-permeable benzophenanthridinone compound that acts as an allosteric and reversible inhibitor of mitochondrial glutaminase activity and represses the growth and invasive activity in glutaminase upregulated fibroblasts and in tumor cells (IC₅₀ ≤ 10 µM in NIH3T3 cells stably expressing Dbl, Cdc42-F28L, Rac-F28L or RhoC-F30L mutants and in SKBR3 and MDA-MB231 cancer cells). Shown to effectively shrink tumor size in P-493 B xenografted mouse model (200 µg per inj. i.p., 12 days).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Wang, J.B., et al. 2010. Cancer Cell18, 207.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Physical form

A 10 mM (5 mg/1.05 ml) sterile-filtered solution of Glutaminase Inhibitor, Compound 968 (Cat. No. 352010) in DMSO.

Reconstitution

Following initial thaw slight warming may be required to resolubilize. Aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)