PJ34

Short Summary : PARP-l inhibitor

Category : Chromatin/Epigenetics|PARP

Purity : 0.98

CAS Number : 344458-19-1

Formula : C17H17N3O2

Molecular Weight : 295.34

SMILE : CN(C)CC(=O)NC1=CC2=C(C=C1)NC(=O)C3=CC=CC=C32

Solubility : Soluble in DMSO > 10 mM

Storage : Store at -20°C

Description : 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

Download datasheet