N-(6-Oxo-5,6-dihydrophenanthridin-2-yl)-2-(N,N-dimethylamino)acetamide
PJ34
CAS: 344458-19-1
Molecular Formula: C17H17N3O2
N-(6-Oxo-5,6-dihydrophenanthridin-2-yl)-2-(N,N-dimethylamino)acetamide - Names and Identifiers
N-(6-Oxo-5,6-dihydrophenanthridin-2-yl)-2-(N,N-dimethylamino)acetamide - Physico-chemical Properties
| Molecular Formula | C17H17N3O2 |
| Molar Mass | 295.34 |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| Use | PJ34 is a potent and specific PARPl/2 inhibitor with IC50 of 110 nM and 86 nM, respectively. |
| In vitro study | PJ34 inhibits the PARP enzyme activity with an IC 50 of 110±1.9 nM. To compare the neuroprotective properties of other PARP inhibitors in PC12 cells, PJ34 is evaluated using by LDH assay. PJ34 treatment also significantly and concentration dependently attenuates cell death at a concentration ranging from 10 -7 to 10 -5 M. |
| In vivo study | To compare the potency and efficacy with other PARP inhibitors, PJ34 is evaluated at the doses of 3.2 and 10 mg/kg, respectively. PJ34 at the dose of 3.2 mg/kg significantly reduces cortical damage by 33%; however, 10 mg/kg dosing shows reversed effect (17% reduction). PJ34 (25 mg/kg) reduces the levels of TNF-α mRNA in ischemic animals by 70% and these values in treated mice do not differ from that of sham or naive animals. Treatment of ischemic mice with PJ34 reduces the level of E-selectin mRNA by 81% and that of ICAM-1 mRNA by 54%, compared to vehicle-treated ischemic mice. |
N-(6-Oxo-5,6-dihydrophenanthridin-2-yl)-2-(N,N-dimethylamino)acetamide - Reference Information
| biological activity | PJ34 is an effective specific PARPl/2 inhibitor with IC50 of 110 nM and 86 nM respectively. |
| target | PARP 110 nM (IC 50 ) PARP-2 86 nM (IC 50 ) PARP-1 110 nM (IC 50 ) |
| in vitro study | PJ34 inhibits the PARP enzyme activity with an IC 50 of 110±1.9 nM. To compare the neuroprotective properties of other PARP inhibitors in PC12 cells, PJ34 is evaluated using by LDH say. PJ34 treatment also significantly and concentration dependently attenuates cell death at a concentration ranging from 10 -7 to 10 -5 m. |
| in vivo research | to compare the potency and efficacy with other PARP inhibitors, PJ34 is evaluated at the doses of 3.2 and 10 mg/kg, respectively. PJ34 at the dose of 3.2 mg/kg significantly reduces cortical damage by 33%; however, 10 mg/kg dosing shows reversed effect (17% reduction). PJ34 (25 mg/kg) reduces the levels of TNF-α mRNA in ischemic animals by 70% and these values in treated mice do not separate from that of sham or naive animals. Treatment of ischemic mice with PJ34 reduces the level of E-selectin mRNA by 81% and that of ICAM-1 mRNA by 54%, compared to vehicle-treated ischemic mice. |
Last Update：2024-04-09 21:11:58
