"目录号: HY-13688A
Cell Cycle/DNA DamageEpigenetics-
PJ34 是一种有效的特异性PARPl/2抑制剂，IC50分别为 110 nM 和 86 nM。
相关产品
Olaparib-BMN-673-MK-4827-XAV-939-Rucaparib phosphate-Nicotinamide-PJ34 hydrochloride-Veliparib dihydrochloride-NVP-TNKS656-AZD-2461-E7449-BSI-201-G007-LK-INO-1001-A-966492-
生物活性
Description
PJ34 is a potent specific inhibitor ofPARPl/2withIC50of 110 nM and 86 nM, respectively.
IC50& Target
IC50: 110 nM (PARP1), 86 nM (PARP2)[1]
In Vitro
PJ34 inhibits the PARP enzyme activity with an IC50of 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 10-7to 10-5M[1].
In Vivo
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)[1]. 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[2].
References
