5.06073
Glutaminase Inhibitor, Compound 968
InSolution
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
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About This Item
Empirical Formula (Hill Notation):
C27H27BrN2O
Molecular Weight:
475.42
NACRES:
NA.77
UNSPSC Code:
12352202
Quality Segment
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
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
mitochondrial glutaminase
Reversible: yes
Packaging
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.
Preparation Note
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
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
10 - Combustible liquids
wgk
WGK 2
flash_point_f
188.6 °F - (refers to pure substance)
flash_point_c
87 °C - (refers to pure substance)
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