PARP-l inhibitor
CAS：344458-19-1
分子式：C17H17N3O2
分子量：295.34
纯度：98%
存储：Store at -20°C

Background:

IC50 Value: 20 nM(EC50)[1] PJ34 (hydrochloride) is a novel potent specific inhibitor of PARP-l. PJ34 has been reported to enhance chemotherapeutic effects in certain types of tumors. 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]. 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]. Clinical trial: N/A