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| Glutaminase C-IN-1 Basic information |
| Product Name: | Glutaminase C-IN-1 | | Synonyms: | 5-[3-BroMo-4-(diMethylaMino)phenyl]-2,3,5,6-tetrahydro-2,2-diMethylbenzo[a]phenanthridin-4(1H)-one;Glutaminase C-IN-1;Glutaminase C-IN-1 (968);Glutaminase Inhibitor Compound 968;glutaminase inhibitor 968;CS-2083;5-[3-bromo-4-(dimethylamino)phenyl]-2,2-dimethyl-1,3,5,6-tetrahydrobenzo[a]phenanthridin-4-one;Glutaminase C inhibitor 1 | | CAS: | 311795-38-7 | | MF: | C27H27BrN2O | | MW: | 475.42 | | EINECS: | | Product Categories: | | Mol File: | 311795-38-7.mol |
| Glutaminase C-IN-1 Chemical Properties |
| 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. |
| Glutaminase C-IN-1 Usage And Synthesis |
| 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. | | 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. | | 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 |
| Glutaminase C-IN-1 Preparation Products And Raw materials |
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