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Merck

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

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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

InChI key

NVFRRJQWRZFDLM-UHFFFAOYSA-N

Related Categories

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)

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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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