PJ-34 Chemical Properties

storage temp. 

Sealed in dry,Store in freezer, under -20°C

solubility 

Soluble in DMSO

form 

Solid

color 

Light yellow to khaki

PJ-34 Usage And Synthesis

Uses

PJ34 is a potent specific inhibitor of PARPl/2 with IC50 of 110 nM and 86 nM, respectively.

Definition

ChEBI: PJ34 is a member of the class of phenanthridines that is 5,6-dihydrophenanthridine substituted at positions 2 and 6 by (N,N-dimethylglycyl)amino and oxo groups, respectively. It is a potent inhibitor of poly(ADP-ribose) polymerases PARP1 and PARP2 (IC50 of 110 nM and 86 nM, respectively) and exhibits anti-cancer, cardioprotective and neuroprotective properties. It has a role as an EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor, an antineoplastic agent, an apoptosis inducer, an angiogenesis inhibitor, an antiatherosclerotic agent, a cardioprotective agent, an anti-inflammatory agent and a neuroprotective agent. It is a member of phenanthridines, a secondary carboxamide and a tertiary amino compound. It is a conjugate base of a PJ34(1+).

Enzyme inhibitor

This PARP inhibitor (FWfree-base = 295.34 g/mol; FWhydrochloride = 331.80 g/mol), systematically named N-(6-oxo-5,6-dihydro-phenanthridin-2-yl)- N,N-dimethylacetamide and known for its activity in neuroprotection under stress conditions, exclusively eradicates multi-centrosomal human mammary, colon, lung, pancreas, ovarian cancer cells, by acting as an extracentrosome extracentrosome( s) de-clustering agent in mitosis. When applied at 20-30 μM, PJ-34 caused G2/M-arrest and a massive cell death Normal human proliferating endothelial, epithelial and mesenchymal cells were unaffected. PJ-34’s cytotoxicity on cancer cells is not attributable to PARP inhibition alone. PJ-34 was originally designed to protect neuronal cells in the central nervous system from cell death evoked by high activity of PARP-1 in response to DNA damage caused by brain injury, stroke or inflammation. Targets: extra-centrosome de-clustering; polyADP-ribose polymerase-1, EC50 = 20 nM

in vivo

IC 50

PARP: 110 nM (IC₅₀); PARP-2: 86 nM (IC₅₀); PARP-1: 110 nM (IC₅₀)

References

[1] Iwashita A, et al. A novel and potent poly(ADP-ribose) polymerase-1 inhibitor, FR247304 (5-chloro-2-[3-(4-phenyl-3,6-dihydro-1(2H)-pyridinyl)propyl]-4(3H)-quinazolinone), attenuates neuronal damage in in vitro and in vivo models of cerebral ischemia. J Ph DOI:10.1124/jpet.104.066944
[2] Haddad M, et al. Anti-inflammatory effects of PJ34, a poly(ADP-ribose) polymerase inhibitor, in transient focal cerebral ischemia in mice. Br J Pharmacol. 2006 Sep;149(1):23-30. DOI:10.1038/sj.bjp.0706837

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