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Merck
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Key Documents

SML1327

Sigma-Aldrich

Glutaminase Inhibitor 968

≥98% (HPLC)

Sinónimos:

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

Fórmula empírica (notación de Hill):
C27H27BrN2O
Número de CAS:
Peso molecular:
475.42
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 5 mg/mL, clear (warmed)

storage temp.

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

InChI key

NVFRRJQWRZFDLM-UHFFFAOYSA-N

General description

Glutaminase Inhibitor 968 belongs to the benzophenanthridinone family.

Application

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

Biochem/physiol Actions

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.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Visite la Librería de documentos

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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