PJ-34 hydrochloride

• CAT Number: I003256
• CAS Number: 344458-15-7
• Molecular Formula: C₁₇H₁₇N₃O₂.HCl
• Molecular Weight: 331.8
• Purity: ≥95%
• Synonyms: 2-(dimethylamino)-N-(6-oxo-5H-phenanthridin-2-yl)acetamide;hydrochloride
• Target: PARP
• Solubility: DMSO > 35 mg/ml
• Storage: 3 years -20C powder
• IC50: 20 nM(EC50)[1]
• InChI: InChI=1S/C17H17N3O2.ClH.H2O/c1-20(2)10-16(21)18-11-7-8-15-14(9-11)12-5-3-4-6-13(12)17(22)19-15;;/h3-9H,10H2,1-2H3,(H,18,21)(H,19,22);1H;1H2
• InChIKey: YCALIZUKAFUQCH-UHFFFAOYSA-N
• SMILES: CN(C)CC(=O)NC1=CC2=C(C=C1)NC(=O)C3=CC=CC=C32.O.Cl

PJ34 hydrochloride is a novel potent specific inhibitor of PARP-l/2 with EC50 of 20 nM.IC50 Value: 20 nM(EC50)[1]Target: PARP1/2in vitro: PJ34 inhibited peroxynitrite-induced cell necrosis with EC50 of 20 nM. PJ34 provides cardioprotection by decreasing myocardial infarct size and enhancing postischemic regional and global functional recovery [1]. Treatment with PJ34 increased NIS promoter activity without affecting PARP-1 binding to the promoter sequence, in addition to an increase of histone modification activation marks (H3K9K14ac, H3K4me3) [2].in vivo: In a model of systemic endotoxemia, PJ34 pretreatment significantly reduced plasma levels of TNF-alpha, IL-1beta and nitrite/nitrate (breakdown products of nitric oxide) production. PJ34 treatment (oral gavage) induced a significant suppression of the inflammatory response in dextran sulfate colitis, multiple low dose streptozotocin diabetes [3]. The PJ34 showed significant reduction on infarct size (37.5%+/-4.5% and 50.5%+/-4.8% of the area at risk) for PJ34 and control pigs groups, respectively, (p < 0.05) [4].

Reference

[1]. Garcia Soriano F, Virág L, Jagtap P, Diabetic endothelial dysfunction: the role of poly(ADP-ribose) polymerase activation. Nat Med. 2001 Jan;7(1):108-13.
[2]. Lavarone E, Puppin C, Passon N, The PARP inhibitor PJ34 modifies proliferation, NIS expression and epigenetic marks in thyroid cancer cell lines. Mol Cell Endocrinol. 2013 Jan 5;365(1):1-10.
[3]. Mabley JG, Jagtap P, Perretti M, Anti-inflammatory effects of a novel, potent inhibitor of poly (ADP-ribose) polymerase. Inflamm Res. 2001 Nov;50(11):561-9.
[4]. Faro R, Toyoda Y, McCully JD, Myocardial protection by PJ34, a novel potent poly (ADP-ribose) synthetase inhibitor. Ann Thorac Surg. 2002 Feb;73(2):575-81.