5.06073

Glutaminase Inhibitor, Compound 968

InSolution, ≥99%, A cell-permeable benzophenanthridinone compound

• Synonym(s): InSolution Glutaminase Inhibitor, Compound 968, GAC Inhibitor, GLS1 Inhibitor I, KGA Inhibitor I, Kidney-Type Glutaminase Inhibitor I, 5-(3-Bromo-4-(dimethylamino)phenyl)-2,2-dimethyl-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one
• Empirical Formula (Hill Notation): C₂₇H₂₇BrN₂O
• Molecular Weight: 475.42
• UNSPSC Code: 12352202
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥99% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• storage temp.: −70°C

Description

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).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
mitochondrial glutaminase

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

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.

Other Notes

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

Legal Information

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

Safety Information

• Storage Class: 10 - Combustible liquids
• wgk_germany: WGK 2
• flash_point_f: 188.6 °F - (refers to pure substance)
• flash_point_c: 87 °C - (refers to pure substance)