"目錄號(hào): HY-13688A

Cell Cycle/DNA DamageEpigenetics-

PJ34 是一種有效的特異性PARPl/2抑制劑，IC50分別為 110 nM 和 86 nM。

PARP

相關(guān)產(chǎn)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

[1].Iwashita A, et al. A novel and potent poly(ADP-ribose) polymerase-1 inhibitor, FR247304 (5-chloro-2-[3-(4-phenyl-3,6-dihydro-1(2H)-pyridinyl)propyl]-4(3H)-quinazolinone), attenuates neuronal damage in in vitro and in vivo models of cerebral ischemia. J Ph

[2].Haddad M, et al. Anti-inflammatory effects of PJ34, a poly(ADP-ribose) polymerase inhibitor, in transient focal cerebral ischemia in mice. Br J Pharmacol. 2006 Sep;149(1):23-30.