| Identification | Back Directory | [Name]
Glutaminase C-IN-1 | [CAS]
311795-38-7 | [Synonyms]
CS-2083
Compound 968
Glutaminase C-IN-1
Glutaminase C-IN-1 (968)
glutaminase inhibitor 968
Glutaminase C inhibitor 1
Glutaminase Inhibitor Compound 968
Glutaminase Inhibitor 968 >=98% (HPLC)
5-[3-bromo-4-(dimethylamino)phenyl]-2,2-dimethyl-1,3,5,6-tetrahydrobenzo[a]phenanthridin-4-one
5-[3-BroMo-4-(diMethylaMino)phenyl]-2,3,5,6-tetrahydro-2,2-diMethylbenzo[a]phenanthridin-4(1H)-one
Benzo[a]phenanthridin-4(1H)-one, 5-[3-bromo-4-(dimethylamino)phenyl]-2,3,5,6-tetrahydro-2,2-dimethyl- | [Molecular Formula]
C27H27BrN2O | [MDL Number]
MFCD00606231 | [MOL File]
311795-38-7.mol | [Molecular Weight]
475.42 |
| Chemical Properties | Back Directory | [Boiling point ]
623.2±55.0 °C(Predicted) | [density ]
1.39±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
Soluble in DMSO (up to 11 mg/ml) or in Ethanol (up to 1 mg/ml with warming) | [form ]
powder | [pka]
4.09±0.42(Predicted) | [color ]
white to beige | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [Description]
GAC Inhibitor 968 (311795-38-7) is an allosteric inhibitor of glutaminase C (GAC).1 Inhibition of GAC blocks oncogenic transformation induced by Rho GTPases in fibroblasts and B lymphoma cells with no effect on normal cells.2 Inhibits liver-type glutaminase GLS2 and suppresses breast tumor growth in vivo.3,4 Reverses acquired erlotinib resistance in non-small cell lung cancer.5 | [Uses]
Glutaminase inhibitor 968 has been used to study the role of glutamine metabolism in macrophage activation. | [Definition]
ChEBI: 5-[3-bromo-4-(dimethylamino)phenyl]-2,2-dimethyl-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one is a partially hydrogenated benzophenanthridine carrying an oxo group at C-4, geminal methyl groups at C-2 and a 3-bromo-4-(dimethylamino)phenyl group at C-5. It has a role as an EC 3.5.1.2 (glutaminase) inhibitor. | [General Description]
Glutaminase Inhibitor 968 belongs to the benzophenanthridinone family. | [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. | [storage]
Store at -20°C | [References]
Stainecker et al. (2015), Mechanism by which a recently discovered allosteric inhibitor blocks glutamine metabolism in transformed cells; Proc. Natl. Acad. Sci. USA, 112 394
Wang et al. (2010), Targeting mitochondrial glutaminase activity inhibits oncogenic transformation; Cancer Cell, 18 207
Katt et al. (2012), Dibenzophenanthridines as inhibitors of glutaminase C and cancer cell proliferation; Cancer Ther., 11 1269
Lukey et al. (2019), Liver-Type Glutaminase GLS2 Is a Druggable Metabolic Node in Luminal-Subtype Breast Cancer; Cell Reports, 29 76
Xie et al. (2016), Inhibition of mitochondrial glutaminase activity reverses acquired erlotinib resistance in non-small cell lung cancer; Oncotarget, 7 610 |
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Sigma-Aldrich
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021-61415566 800-8193336 |
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https://www.sigmaaldrich.cn |
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