| 货号 | 14440-1mg |
| 描述 | The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis, particularly in response to reactive oxygen and nitrogen species.1,2 PJ-34 is an inhibitor of PARPs which can be used in cells or in animals.3,4,5 It binds and inhibits the PARP tankyrase1 (IC50 = 1 μM).6 PJ-34 also inhibits matrix metalloproteinase-2 when used at higher concentrations (IC50 = 56 μM).7 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Davar, D.,Beumer, J.H.,Hamieh, L., et al. Role of PARP inhibitors in cancer biology and therapy. Current Medicinal Chemistry 19(23), 3907-3921 (2012). 2.Mathews, M.T. and Berk, B.C. PARP-1 inhibition prevents oxidative and nitrosative stress-induced endothelial cell death via transactivation of the VEGF receptor 2. Arteriosclerosis, Thrombosis, and Vascular Biology 28, 711-717 (2008). 3.Soriano, F.G.,Pacher, P.,Mabley, J., et al. Rapid reversal of the diabetic endothelial dysfunction by pharmacological inhibition of poly(ADP-ribose) polymerase. Circulation Research 89(8), 684-691 (2001). 4.Fonfria, E.,Marshall, I.C.B.,Benham, C.D., et al. TRPM2 channel opening in response to oxidative stress is dependent on activation of poly(ADP-ribose) polymerase. British Journal of Pharmacology 143, 186-192 (2004). 5.Radnai, B.,Antus, C.,Racz, B., et al. Protective effect of the poly(ADP-ribose) polymerase inhibitor PJ34 on mitochondrial depolarization-mediated cell death in hepatocellular carcinoma cells involves attenuation of c-Jun N-terminal kinase-2 and protein kinase B/Akt activation. Molecular Cancer 11(34), (2012). 6.Kirby, C.A.,Cheung, A.,Fazal, A., et al. Structure of human tankyrase 1 in complex with small-molecule inhibitors PJ34 and XAV939. Acta Crystallogr.Sect.F Struct.Biol.Cryst.Commun. 68, 115-118 (2012). 7.Nicolescu, A.C.,Holt, A.,Kandasamy, A.D., et al. Inhibition of matrix metalloproteinase-2 by PARP inhibitors. Biochemical and Biophysical Research Communications 387(4), 646-650 (2009). | |
| 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 | 331.8 |
| 分子式 | C17H17N3O2 • HCl |
| CAS号 | 344458-15-7 |
| 稳定性 | ≥ 2 years |
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