<p style=/line-height:25px/>PJ34 hydrochloride is a novel potent specific inhibitor of PARP-l/2 with EC50 of 20 nM.<br>IC50 Value: 20 nM(EC50)[1]<br>Target: PARP1/2<br>in 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].<br>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].<br></p>
| Catalog Number | I003256 |
| CAS Number | 344458-15-7 |
| Synonyms | 2-(dimethylamino)-N-(6-oxo-5H-phenanthridin-2-yl)acetamide;hydrochloride |
| Molecular Formula | C₁₇H₁₇N₃O₂.HCl |
| Purity | ≥95% |
| 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 |
| Reference | <p style=/line-height:25px/> |
