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352010

Sigma-Aldrich

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

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About This Item

Empirical Formula (Hill Notation):
C27H27BrN2O
CAS Number:
311795-38-7
Molecular Weight:
475.42
MDL number:
MFCD00606231
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

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

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).
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. 506073).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

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

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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