product name PJ34 HCl
Description: PJ34 is a novel and potent inhibitor of poly(ADP-ribose) polymerase (PARP) that dose-dependently inhibits purified PARP enzyme in a cell-free assay with an 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.
References: Nat Med. 2001 Jan;7(1):108-13; J Pharmacol Exp Ther. 2004 Sep;310(3):1053-61.
331.8
Formula
C17H17N3O2.HCl
CAS No.
344458-15-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 66 mg/mL (198.9 mM)
Water: 66 mg/mL (198.9 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
30% PEG400+0.5% Tween80+5% propylene glycol: 14 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: PJ34 is a potent, phenanthridinone PARS inhibitor, which is approximately 10,000 times more potent than the prototypical PARS inhibitor 3-aminobenzamide. PJ34 inhibited peroxynitrite-induced cell necrosis with EC50 of 20 nM. PJ34 provides cardioprotection by decreasing myocardial infarct size and enhancing postischemic regional and global functional recovery. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | PJ34 suppresses the development of clinical signs of EAE in MBP-immunized PLSJL mice. PJ34 exerted therapeutic effects at the onset of EAE that are associated with reduced CNS inflammation and the maintenance of neurovascular integrity. PJ34 partially inhibits the expression of TNF-α and ICAM-1 in the Spinal Cord Tissues of MBP-Immunized Mice. PJ34 provides significant, dose-dependent, anti-inflammatory effects in a variety of local inflammation models. PJ34 dose-dependently suppresses neutrophil infiltration and nitric oxide (but not KC and IL-1β) production in peritonitis. In a model of systemic endotoxemia, PJ34 pretreatment significantly reduces plasma levels of TNF-α, IL-1β and nitrite/nitrate (breakdown products of nitric oxide) production. PJ34 treatment (oral gavage) induces a significant suppression of the inflammatory response in dextran sulfate colitis, multiple low dose streptozotocin diabetes and cyclophosphamide-accelerated autoimmune diabetes in the non-obese diabetic mice, and reduces the degree of mononuclear cell infiltration into the iris in an endotoxin-induced uveitis model. |
| Animal model | Female PLSJL mice |
| Formulation & Dosage | Dissolved in saline; 10 mg/kg; Oral administration |
| References | Inflamm Res. 2001 Nov;50(11):561-9; Nat Med. 2001 Jan;7(1):108-13; J Pharmacol Exp Ther. 2004 Sep;310(3):1053-61. |
