| 货号 | 14192-1mg |
| 描述 | PX 12 is a competitive, irreversible inhibitor of thioredoxin 1 (Trx1), acting by binding to Cys73 of this enzyme.1 As Trx1 is overexpressed in certain cancers, PX 12 is effective in suppressing the growth of cancer cells, with growth inhibition in a panel of 60 human tumors significantly correlated with expression of Trx1 mRNA.2,3 Through its effects on Trx1, PX 12 reduces hypoxia-induced HIF-1α protein levels (IC50 = 7.2 μM), as well as expression of VEGF (IC50 = 10.4 μM) and iNOS (IC50 = 18.1 μM), culminating in attenuation of the proliferation of MCF-7 cells (IC50 = 1.9 μM) and HT-29 cells (IC50 = 2.9 μM) as well as reduced microvessel density in MCF-7 tumor xenografts.4 PX 12 also blocks Trx-mediated activation of extracellular transglutaminase 2 (IC50 = ~3 μM) and Trx-1-increased expression and translation of CYP1B1.5,6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Oblong, J.E.,Chantler, E.L.,Gallegos, A., et al. Reversible inhibition of human thioredoxin reductase activity by cytotoxic alkyl 2-imidazolyl disulfide analogues. Cancer Chemotherapy and Pharmacology 34, 434-438 (1994). 2.Powis, G. and Montfort, W.R. Properties and biological activities of thioredoxins. Annual Reviews of Biophysical and Biomolecular Structure 30, 421-455 (2001). 3.Mukherjee, A. and Martin, S.G. The thioredoxin system: A key target in tumour and endothelial cells. Br.J.Radiol. 81, S57-S68 (2008). 4.Welsh, S.J.,Williams, R.R.,Birmingham, A., et al. The thioredoxin redox inhibitors 1-methylpropyl 2-imidazolyl disulfide and pleurotin inhibit hypoxia-induced factor 1α and vascular endothelial growth factor formation. Molecular Cancer Therapeutics 2(3), 235-243 (2003). 5.Jin, X.,Stamnaes, J.,Klöck, C., et al. Activation of extracellular transglutaminase 2 by thioredoxin. The Journal of Biological Chemisty 286(43), 37866-37873 (2011). 6.Husbeck, B. and Powis, G. The redox protein thioredoxin-1 regulates the constitutive and inducible expression of the estrogen metabolizing cytochromes P450 1B1 and 1A1 in MCF-7 human breast cancer cells. Carcinogenesis 23(10), 1625-1630 (2002). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 188.3 |
| 分子式 | C7H12N2S2 |
| CAS号 | 141400-58-0 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |