PJ34 hydrochloride 是一种PARP1/2的特异性有效抑制剂，IC50值分别为 110 nM 和 86 nM。

PJ34 hydrochloride is a potent specific inhibitor of PARPl/2.

在MBP免疫的PLSJL小鼠中,PJ34部分抑制脊髓组织中TNF-α和ICAM-1的表达,抑制EAE的临床体征的发展.在全身性内毒素血症模型中,PJ34能够减低血浆TNF-α,IL-1β和亚硝酸盐/硝酸盐的含量. 在非肥胖糖尿病小鼠中,强饲口服PJ34能够抑制硫酸葡聚糖结肠炎反应.

在过氧亚硝酸盐诱导的细胞中（EC 50=20 nM）,PJ34能够抑制细胞坏死的发生。

To assess the PARP-1 or PARP-2 inhibitory activity of FR247304, 3-AB, and PJ34, PARP activity is evaluated with minor modifications. PARP enzyme assay is carried out in a final volume of 100 μL consisting of 50 mM Tris-HCl (pH 8.0), 25 mM MgCl2, 1 mM dithiothreitol, 10 μg activated salmon sperm DNA, 0.1 μCi of [adenylate-32P]NAD, 0.2 units of recombinant human PARP for PARP-1 assay or 0.1 units of recombinant mouse PARP-2 for PARP-2 assay, and various concentrations of FR261529 or 3-AB. The reaction mixture is incubated at room temperature (23°C) for 15 min, and the reaction is terminated by adding 200 μL of ice-cold 20% trichloroacetic acid (TCA) and incubated at 4°C for 10 min. The precipitate is transferred onto GF/B filter and washed three times with 10% TCA solution and 70% ethanol. After the filter is dried, the radioactivity is determined by liquid scintillation counting.

PJ34 is dissolved in 100% DMSO at 10 mM and then diluted in DMEM without serum[1]. PC12 cell cultured are grown in Dulbecco's modified Eagle's medium supplemented with 5% (v/v) fetal calf serum, 5% (v/v) horse serum, and a 1% (v/v) penicillin-streptomycin antibiotics mixture. Cells are grown in an atmosphere of 95% air and 5% CO2 at 37°C. For all experiment, cells are seeded at a density of 4×104 cells/well in 96-well culture plates and allowed to attach overnight. For assessment of cell viability, hydrogen peroxide-induced cytotoxicity is quantified by a standard measurement of LDH release with the use of the LDH assay kit. Briefly, 6 h after hydrogen peroxide exposure, 20 μL of medium of each well is collected, and the solution prepared from LDH assay kit is added. After incubation at room temperature for 30 min, the reaction is stopped by addition of 1 N HCl, and absorbance is measured at 450 nm using a microplate reader.

344458-15-7

C17H18ClN3O2

331.8

PJ34 HCl

DMSO:33.2 mg/mL (100 mM)
H2O:33.2 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years