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PJ34PARP-l inhibitor

PJ34

Catalog No. A3729
Size Price Stock Qty
5mg $50.00 In stock
10mg $60.00 In stock
50mg $170.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

PJ34

Related Biological Data

PJ34

Related Biological Data

PJ34

Biological Activity

PJ34 is a novel potent specific inhibitor of PARP-l/2 with EC50 of 20 nM.
Targets PARP          
IC50 20 nM (EC50)          

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Chemical Properties

Cas No. 344458-19-1 SDF Download SDF
Synonyms PJ-34;PJ 34
Chemical Name 2-(dimethylamino)-N-(6-oxo-5H-phenanthridin-2-yl)acetamide
Canonical SMILES CN(C)CC(=O)NC1=CC2=C(C=C1)NC(=O)C3=CC=CC=C32
Formula C17H17N3O2 M.Wt 295.34
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips N/A
Shipping Condition N/A

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