PJ34 hydrochloride
Cat. No.:YN290283
CAS No. :344458-15-7
产品名称: | PJ34 hydrochloride |
CAS No.: | 344458-15-7 |
Chemical Name: | N-(5,6-dihydro-6-oxo-2-phenanthridinyl)-2-(dimethylamino)-acetamide, monohydrochloride |
Synonyms: | PJ34 HCl |
分子量: | 331.80 |
分子式: | C₁₇H₁₈ClN₃O₂ |
SMILES: | O=C(NC(C=C1C2=C3C=CC=C2)=CC=C1NC3=O)CN(C)C.Cl |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | PJ34 hydrochloride 是PARP1/2的抑制剂,IC50值分别为 110 nM 和 86 nM。 |
IC50和靶点: | [{name:"PARP:110 nM (IC50)"},{name: "PARP-2:86 nM (IC50)"},{name: "PARP-1:110 nM (IC50)"}] |
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Davar, D., Beumer, J.H., Hamieh, L., et al.Role of PARP inhibitors in cancer biology and therapyCurr. Med. Chem.19(23),3907-3921(2012)
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 2Arterioscler. Thromb. Vasc. Biol.28,711-717(2008)
Soriano, F.G., Pacher, P., Mabley, J., et al.Rapid reversal of the diabetic endothelial dysfunction by pharmacological inhibition of poly(ADP-ribose) polymeraseCirc. Res.89(8),684-691(2001)
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) polymeraseBr. J. Pharmacol.143,186-192(2004)
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 activationMol. Cancer11(34),(2012)
Kirby, C.A., Cheung, A., Fazal, A., et al.Structure of human tankyrase 1 in complex with small-molecule inhibitors PJ34 and XAV939Acta Crystallogr. Sect. F Struct. Biol. Cryst. Commun.68 (Pt 2),115-118(2012)
Nicolescu, A.C., Holt, A., Kandasamy, A.D., et al.Inhibition of matrix metalloproteinase-2 by PARP inhibitorsBiochem. Biophys. Res. Commun.387(4),646-650(2009)