中文同义词:
N-(6-氧代-5,6-二氢菲啶-2-基)-2-(N,N-二甲基氨基)乙酰胺盐酸盐;PJ 34 盐酸盐;PARPL和PARP2抑制剂
英文同义词:
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
相关类别:
细胞生物学试剂;DNA损伤;小分子抑制剂，天然产物;小分子抑制剂;Amines;Aromatics;Heterocycles;Inhibitors;Intermediates Fine Chemicals;Pharmaceuticals
储存条件
Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
敏感性
Light Sensitive Hygroscopic
生物活性
PJ34 hydrochloride 是 PARP1/2 的抑制剂，IC50 值分别为 110 nM 和 86 nM。
靶点
PARP
110 nM (IC 50 )
PARP-2
86 nM (IC 50 )
PARP-1
110 nM (IC 50 )
PARP
110 nM (IC 50 )
PARP-2
86 nM (IC 50 )
体外研究
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.
体内研究
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.
