352010

Glutaminase Inhibitor, Compound 968

Glutaminase Inhibitor, Compd 968, is a cell-permeable, reversible inhibitor of mitochondrial glutaminase. Represses growth & invasive activity in glutaminase upregulated fibroblasts and tumor cells.

• Synonym(s): 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
• CAS Number: 311795-38-7
• Molecular Weight: 475.42
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD00606231
• Assay: ≥99% (HPLC)
• Form: powder
• Storage condition: OK to freeze, protect from light

Properties

• Quality Segment: 100
• assay: ≥99% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: white
• solubility: DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: O=C(CC(C)(C)C1)C2=C1C3=C(NC2C4=CC(Br)=C(C=C4)N(C)C)C=CC5=C3C=CC=C5
• InChI key: NVFRRJQWRZFDLM-UHFFFAOYSA-N

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). Also available as a 10 mM solution in DMSO (Cat. No. 5.06073).

Packaging

Packaged under inert gas

Other Notes

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

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable