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PJ34 hydrochloridePARP inhibitor,potent and cell-permeable

PJ34 hydrochloride

Catalog No. A4159
Size Price Stock Qty
10mM (in 1mL DMSO) $65.00 In stock
Evaluation Sample $28.00 In stock
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.

Quality Control

Quality Control & MSDS

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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)          

Protocol

Cell experiment [1]:

Cell lines

HepG2 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months.

Reacting condition

0.5, 1.0 and 2.0 mg/L; 9 days

Applications

At the doses of 0.5, 1.0 and 2.0 mg/L, PJ34 significantly inhibited HepG2 cell proliferation on days 6 and 9 of culture.

Animal experiment [1]:

Animal models

Nude mice bearing HepG2-derived tumors

Dosage form

3 mg/kg; i.p.; every other day for 21 days

Applications

PJ34 inhibited HepG2 cell-derived tumor growth in nude mice.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. 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

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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