344458-15-7 Usage
Description
PJ-34, also known as PJ-34 HCl, is a potent and selective inhibitor of poly(ADP-ribose) polymerase (PARP1 and 2) with an EC50 of 20 nM. It is a cell-permeable, water-soluble phenanthridinone-derivative that has been shown to be approximately 10,000 times more potent than the prototypical PARP inhibitor, 3-Aminobenzamide. PJ-34 does not act as an antioxidant at higher concentrations and has demonstrated neuroprotection in both in vivo and in vitro models of stroke.
Uses
1. Used in Anticancer Applications:
PJ-34 is used as a poly adenosine diphosphate-ribose polymerase inhibitor for attenuating chromate-induced nephrotoxicity and has a lethal effect on breast cancer cells, particularly on breast cancer MCF-7, both in vitro and in vivo.
2. Used in Neuropathic Pain Research:
PJ-34 hydrochloride hydrate is used as a PARP inhibitor in rats to test the effect of PARP1 in neuropathic pain.
3. Used in Protein Extraction:
PJ-34 is used as a component of protein extraction buffer to enable the visualization of the high-molecular-weight smear of PARylated proteins in various cell samples.
4. Used in Cell Line Studies:
PJ-34 serves as a PARP inhibitor in the murine MLE-12 epithelial cell line.
5. Used in Ischemia Reperfusion Injury:
PJ-34 HCl reduces ischemia reperfusion injury in a mouse model.
6. Used in Inflammatory Research:
PJ-34 displays anti-inflammatory effects in a transient focal cerebral ischemia mouse model.
7. Used in Cell Cycle Regulation:
PJ-34 HCl causes PARP1 independent, p21 dependent mitotic arrest.
Application Industries:
1. Pharmaceutical Industry: PJ-34 is used in the development of anticancer drugs and therapies.
2. Biotechnology Industry: PJ-34 is utilized in research and development of novel drug delivery systems, protein extraction, and cell line studies.
3. Neuroscience Research: PJ-34 is applied in the study of neuroprotection and neuropathic pain.
4. Inflammatory Disease Research: PJ-34 is used to investigate its anti-inflammatory effects in various disease models.
Biological Activity
Potent inhibitor of poly(ADP-ribose) polymerase (PARP) (EC 50 = 20 nM). ~ 1000-fold more potent than 3-Aminobenzamide . Protects primary neuronal cells from oxygen-glucose deprivation in vitro and reduces infarct size following focal cerebral ischemia in vivo .
Biochem/physiol Actions
Cell permeable: yes
References
1) Pellicciari et al. (2008), On the way to selective PARP-2 inhibitors. Design, synthesis, and preliminary evaluation of a series of isoquinolinone derivatives; Chem. Med. Chem., 3 914
2) Crawford et al. (2010), Postischemic poly (ADP-ribose) polymerase (PARP) inhibition reduces ischemia reperfusion injury in a hind-limb ischemia model; Surgery, 148 110
3) Haddad et al. (2006), Anti-inflammatory effects of PJ34, a poly(ADP-ribose) polymerase inhibitor, in transient focal cerebral ischemia in mice; Br. J. Pharmacol., 149 23
4) Madison et al. (2011), The PARP inhibitor PJ34 causes a PARP1-independent, p21 dependent mitotic arrest; DNA Repair, 10 1003
Check Digit Verification of cas no
The CAS Registry Mumber 344458-15-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,4,4,4,5 and 8 respectively; the second part has 2 digits, 1 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 344458-15:
(8*3)+(7*4)+(6*4)+(5*4)+(4*5)+(3*8)+(2*1)+(1*5)=147
147 % 10 = 7
So 344458-15-7 is a valid CAS Registry Number.
