货号 | 17199-1mg |
描述 | Glutaminase inhibitor compound 968 is a cell-permeable, reversible inhibitor of a mitochrondrial glutaminase splice variant, glutaminase C (IC50 = ~2.5 µM), which is commonly found in cancer cells.1,2 Through this action, glutaminase inhibitor compound 968 blocks transformation induced by Rho GTPases and inhibits the proliferation of non-invasive epithelial (T-47D and MDA-MB-361) and invasive mesenchymal (MDA-MB-231 and Hs578T) cancer cells, without affecting normal cells.2,3,4 Glutaminase inhibitor compound 968 induces apoptosis and alters both histone methylation and gene expression in cancer cells.4 |
供应商 | Cayman |
应用文献 | |
1.Stalnecker, C.A.,Ulrich, S.M.,Li, Y., et al. Mechanism by which a recently discovered allosteric inhibitor blocks glutamine metabolism in transformed cells. Proc.Natl.Acad.Sci. USA 112(2), 394-399 (2015). 2.Wang, J.-B.,Erickson, J.W.,Fuji, R., et al. Targeting mitochondrial glutaminase activity inhibits oncogenic transformation. Cancer Cell 18(3), 2007-2219 (2010). 3.Katt, W.P.,Ramachandran, S.,Erickson, J.W., et al. Dibenzophenanthridines as inhibitors of glutaminase C and cancer cell proliferation. Mol.Cancer Ther. 11(6), 1269-1278 (2012). 4.Simpson, N.E.,Tryndyak, V.P.,Pogribna, M., et al. Modifying metabolically sensitive histone marks by inhibiting glutamine metabolism affects gene expression and alters cancer cell phenotype. Epigenetics 7(12), 1413-1420 (2012). | |
运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 475.4 |
分子式 | C27H27BrN2O |
CAS号 | 311795-38-7 |
稳定性 | ≥ 2 years |
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