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Key Documents

SML1327

Sigma-Aldrich

Glutaminase Inhibitor 968

≥98% (HPLC)

Sinonimo/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

Formula empirica (notazione di Hill):
C27H27BrN2O
Numero CAS:
Peso molecolare:
475.42
Codice UNSPSC:
12352200
NACRES:
NA.77

Livello qualitativo

Saggio

≥98% (HPLC)

Forma fisica

powder

Colore

white to beige

Solubilità

DMSO: 5 mg/mL, clear (warmed)

Temperatura di conservazione

2-8°C

InChI

1S/C27H27BrN2O/c1-27(2)14-19-24-18-8-6-5-7-16(18)9-11-21(24)29-26(25(19)23(31)15-27)17-10-12-22(30(3)4)20(28)13-17/h5-13,26,29H,14-15H2,1-4H3
NVFRRJQWRZFDLM-UHFFFAOYSA-N

Descrizione generale

Glutaminase Inhibitor 968 belongs to the benzophenanthridinone family.

Applicazioni

Glutaminase inhibitor 968 has been used to study the role of glutamine metabolism in macrophage activation.

Azioni biochim/fisiol

Glutaminase Inhibitor 968 is an allosteric inihibitor of the mitochondrial enzyme glutaminase C (GAC), which is overexpressed in a number of cancer cell lines. Glutaminase Inhibitor 968 shows 21% inhibition at 10 μM, 94% at 25 μM. Glutaminase Inhibitor 968 blocked human cancer cell proliferation in culture, and in inhibited tumor formation in mouse xenograft models.
Variation in the 3-bromo-4-(dimethylamino)phenyl ring of glutaminase inhibitor 968, leads to loss of its inhibitory activity. Glutaminase catalysed glutamine metabolism maintains intracellular pH of cancer cells. Inhibition by glutaminase inhibitor 968 is known to hinder cell proliferation as a consequences of low intracellular pH.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


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Glutaminase: a hot spot for regulation of cancer cell metabolism?.
Erickson J W and Cerione R A
Oncotarget, 1(8), 734-734 (2010)
Glutaminase regulation in cancer cells: a druggable chain of events.
Katt W P and Cerione R A
Drug Discovery Today, 19(4), 450-457 (2014)
α-ketoglutarate orchestrates macrophage activation through metabolic and epigenetic reprogramming.
Liu P S, et al.
Nature Immunology, 18(9), 985-985 (2017)
Dibenzophenanthridines as Inhibitors of Glutaminase C and Cancer Cell Proliferation
Katt W P, et al.
Molecular Cancer Therapeutics, 11(6) (2012)
Meijian Liao et al.
EBioMedicine, 41, 200-213 (2019-02-24)
LncRNAs have been found to be involved in various aspects of biological processes. In this study, we aimed to uncover the molecular mechanisms of lncRNA EPB41L4A-AS1 in regulating glycolysis and glutaminolysis in cancer cells. The expression of EPB41L4A-AS1 in cancer

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