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PJ34 hydrochloridePARP inhibitor,potent and cell-permeable

PJ34 hydrochloride

Catalog No. A4159
Size Price Stock Qty
Evaluation Sample $28.00 In stock
5mg $45.00 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 hydrochloride

Related Biological Data

PJ34 hydrochloride

Related Biological Data

PJ34 hydrochloride

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. 344458-15-7 SDF Download SDF
Synonyms PJ 34 Hydrochloride
Chemical Name 2-(dimethylamino)-N-(6-oxo-5H-phenanthridin-2-yl)acetamide;hydrochloride
Canonical SMILES CN(C)CC(=O)NC1=CC2=C(C=C1)NC(=O)C3=CC=CC=C32.Cl
Formula C17H17N3O2.HCl M.Wt 331.8
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

PJ34 is a novel and potent inhibitor of poly(ADP-ribose) polymerase (PARP), an enzyme involved in DNA repair and cell proliferation, that dose-dependently inhibits purified PARP enzyme in a cell-free assay with half maximal effective concentration EC50 value of 20 nM. Unlike other PARP inhibitors (such as 3-AB), PJ34 does not possess any antioxidant properties but exhibits 10,000 times greater PARP inhibition than 3-AB (EC50 = 200 μM). PJ34 has been found to have neuro-protective effects and enhance the chemotherapeutic effects in several tumor types. Study results have shown that PJ34 inhibits peroxynitrite-induced cell necrosis with EC50 value of 20 nM and dose-dependently suppresses the growth of HepG2 cells.

Reference

Sheng-Hui Huang, Min Xiong, Xiao-Ping Chen, Zhen-Yu Xiao, Yin-Feng Zhao and Zhi-Yong Huang. PJ34, an inhibitor of PARP-1, suppresses cell growth and enhances the suppressive effects of cisplatin in liver cancer cells. Oncology Reports 20: 567-572, 2008

Galaleldin E. Abdelkarim, Karen Gertz, Christoph Harms, Juri Katchanov, Ulrich Dirnagl, Csaba Szabo and Matthias Enders. Protective effects of PJ34, a novel, potent inhibitor of poly(ADP-ribose) polymerase (PARP) in in vitro and in vivo models of stroke. International Journal of Molecular Medicine 7: 255-260, 2001