An inhibitor of poly (ADP-ribose) polymerases
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
[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
[2].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
| Cell experiment [1]: | |
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Cell lines |
HepG2 cells |
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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. |
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Reaction Conditions |
0.5, 1.0 and 2.0 mg/L; 9 days |
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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]: | |
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Animal models |
Nude mice bearing HepG2-derived tumors |
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Dosage form |
3 mg/kg; i.p.; every other day for 21 days |
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Applications |
PJ34 inhibited HepG2 cell-derived tumor growth in nude mice. |
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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. |
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参考文献: [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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