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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.

Synonyme(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

Formule empirique (notation de Hill):
C27H27BrN2O
Numéro CAS:
311795-38-7
Poids moléculaire :
475.42
Numéro MDL:
MFCD00606231
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥99% (HPLC)

Forme

powder

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
protect from light

Couleur

white

Solubilité

DMSO: 5 mg/mL

Conditions d'expédition

ambient

Température de stockage

−20°C

Chaîne SMILES 

O=C(CC(C)(C)C1)C2=C1C3=C(NC2C4=CC(Br)=C(C=C4)N(C)C)C=CC5=C3C=CC=C5

Description générale

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).

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Autres remarques

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

Informations légales

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

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Ying Zhang et al.
Oxidative medicine and cellular longevity, 2023, 9808100-9808100 (2023-01-20)
Ferroptosis, a newly identified form of cell death, plays critical roles in the development and chemoresistance of lung cancer. Tripartite motif 6 (TRIM6) acts as an E3-ubiquitin ligase and can promote the progression of human colorectal cancer. The present study
Hamed Alborzinia et al.
Nature cancer, 3(4), 471-485 (2022-04-29)
Aberrant expression of MYC transcription factor family members predicts poor clinical outcome in many human cancers. Oncogenic MYC profoundly alters metabolism and mediates an antioxidant response to maintain redox balance. Here we show that MYCN induces massive lipid peroxidation on
Katharina Koch et al.
Cell death discovery, 6, 20-20 (2020-04-28)
Cancer cells upregulate anabolic processes to maintain high rates of cellular turnover. Limiting the supply of macromolecular precursors by targeting enzymes involved in biosynthesis is a promising strategy in cancer therapy. Several tumors excessively metabolize glutamine to generate precursors for
Kexin Zhang et al.
Molecular carcinogenesis, 57(11), 1566-1576 (2018-07-24)
Ferroptosis is a recently recognized form of regulated cell death driven by lipid-based reactive oxygen species (ROS) accumulation. However, the molecular mechanisms of ferroptosis regulation are still largely unknown. Here we identified a novel miRNA, miR-9, as an important regulator
Luca Simula et al.
Nature communications, 15(1), 2203-2203 (2024-03-12)
The ability of CD8+ T cells to infiltrate solid tumors and reach cancer cells is associated with improved patient survival and responses to immunotherapy. Thus, identifying the factors controlling T cell migration in tumors is critical, so that strategies to
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