PJ-34
PJ-34 Basic information
- Product Name:
- PJ-34
- Synonyms:
-
- PJ 34 Hydrochloride
- N-(5,6-Dihydro-6-oxo-2-phenanthridinyl)-2-acetamidehydrochloride
- PARP Inhibitor VIII, PJ34
- PJ-34 hydrate hydrochloride
- CS-723
- PJ 34;PJ-34
- PI34
- 2-(dimethylamino)-N-(6-oxo-5H-phenanthridin-2-yl)acetamide,hydrochloride
- CAS:
- 344458-15-7
- MF:
- C17H17N3O2HCl
- MW:
- 0
- Product Categories:
-
- Amines
- Aromatics
- Heterocycles
- Inhibitors
- Intermediates & Fine Chemicals
- Pharmaceuticals
- Mol File:
- 344458-15-7.mol
PJ-34 Chemical Properties
- storage temp.
- Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
- solubility
- H2O: soluble22mg/mL
- form
- White solid
- color
- white to yellow
- Sensitive
- Light Sensitive & Hygroscopic
- Stability:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 3 months.
Safety Information
- Safety Statements
- 22-24/25
- WGK Germany
- 3
- HS Code
- 29339900
PJ-34 Usage And Synthesis
Description
PJ-34 HCl (344458-15-7) is a potent and selective inhibitor of PARP1 and 2. EC50 = 20 nM.1?Reduces ischemia reperfusion injury in a mouse model.2 Displays anti-inflammatory effects in a transient focal cerebral ischemia mouse model.3 PJ-34 HCl causes PARP1 independent, p21 dependent mitotic arrest.4
Uses
A poly adenosine diphosphate-ribose polymerase inhibitor, attenuates chromate-induced nephrotoxicity. PJ-34 has a lethal effect on breast cancer cells, both in vitro and in vivo, in particular on breast cancer MCF-7.
Uses
PJ-34 hydrochloride hydrate has been used:
- as a poly(ADP-ribose) polymerase (PARP) inhibitor 1 in rats to test the effect of PAPR1 in neuropathic pain
- as a component of protein extraction buffer to enable visualization of the high-molecular-weight smear of PARylated proteins in various cell samples
- as PARP inhibitor in murine MLE-12 epithelial cell line
Definition
ChEBI: PJ34 hydrochloride is a hydrochloride salt prepared from equimolar amounts of PJ34 and hydrochloric acid. It has a role as an angiogenesis inhibitor, an anti-inflammatory agent, an antiatherosclerotic agent, an antineoplastic agent, an apoptosis inducer, a cardioprotective agent, an EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor and a neuroprotective agent. It contains a PJ34(1+).
General Description
A cell-permeable, water-soluble phenanthridinone-derivative that acts as a potent inhibitor of poly(ADP-ribose) polymerase (PARP; EC50 = 20 nM). Shown to be about 10,000 times more potent than the prototypical PARP inhibitor, 3-Aminobenzamide (Cat. No. 165350; EC50 = 200 μM). Does not act as an antioxidant at higher concentrations (1 μM to 10 mM). Exhibits neuroprotection in in vivo and in vitro models of stroke. Also available as a 20 mM solution in H2O(Cat. No. 528151).
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
storage
+4°C
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
PJ-34Supplier
- Tel
- sales@boylechem.com
- Tel
- 010-82848833 400-666-7788
- jkinfo@jkchemical.com
- Tel
- 821-50328103-801 18930552037
- 3bsc@sina.com
- Tel
- 0330-2528181
- sales@vdmbio.com
- Tel
- 021-50135380
- shchemsky@sina.com
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- 2'-METHYL-BIPHENYL-2-YLAMINE
- N-(6-OXO-5,6-DIHYDRO-PHENANTHRIDIN-2-YL)-N,N DIMETHYLACETAMIDE HYDROCHLORIDE HYDRATE