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PJ34 HCl

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Chemical Structure| 344458-15-7 同义名 : PJ-34 (hydrochloride);PJ34 hydrochloride
CAS号 : 344458-15-7
货号 : A103485
分子式 : C17H18ClN3O2
纯度 : 99%+
分子量 : 331.797
MDL号 : MFCD16618379
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 9 mg/mL(27.13 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(150.69 mM)，配合低频超声助溶
动物实验配方：

30% PEG400+0.5% Tween80+5% propylene glycol+water 15 mg/mL suspension

生物活性
靶点

  • PARP

    PARP, EC50:20 nM
描述 PJ34 is a specific inhibitor of poly (ADP-ribose) polymerase 1, and is involved in immune regulation, may be effective in preventing acute cardiac rejection. Compared with the control group, In vitro, PJ34 (20 mg/kg/day) treatment reduced the proportion of CD4+ IFN-γ+ and CD4+ IL-17A+ cells and increased the percent of CD4+ IL-4+ and CD4+ Foxp3+ cells in the spleens. In vitro, PJ34 treatment significantly inhibited the mRNA levels of IFN-γ and IL-17A and promoted the mRNA levels of TGF-β and FOXP-3 in activated CD4+ T cells[3]. In vivo, PJ34 (20 mg/kg/day) prevented HFD-induced atherosclerosis in the rabbits[4].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
Escherichia coli BL21 Star (DE3) cells Function assay Inhibition of 6xhis-tagged ARTD5 (unknown origin) expressed in Escherichia coli BL21 Star (DE3) cells, IC50=0.57 μM 24900770
Escherichia coli Rosetta2 (DE3) cells Function assay Inhibition of human N-terminal 6xhis-tagged ARTD6 (873 to 1161) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate by fluorescence assay, IC50=0.21878 μM 24900770
HeLa cells Function assay Inhibition of PARP1 in human HeLa cells by fluid scintillation counting using [adenylated-32P]NAD as substrate, IC50=0.02 μM 18713665
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.01mL

0.60mL

0.30mL

15.07mL

3.01mL

1.51mL

30.14mL

6.03mL

3.01mL
参考文献

[1]Scott GS, Kean RB, et al. The therapeutic effects of PJ34 [N-(6-oxo-5,6-dihydrophenanthridin-2-yl)-N,N-dimethylacetamide.HCl] , a selective inhibitor of poly(ADP-ribose) polymerase, in experimental allergic encephalomyelitis are associated with immunomodulation. J Pharmacol Exp Ther. 2004 Sep;310(3):1053-61.

[2]Scott GS, et al. J Pharmacol Exp Ther, 2004, 310(3), 1053-1061.

[3]Chen X, Huang Y, Wang D, Dong N, Du X. PJ34, a PARP1 inhibitor, attenuates acute allograft rejection after murine heart transplantation via regulating the CD4+ T lymphocyte response. Transpl Int. 2021;34(3):561-571.

[4]Zha S, Wang F, Li Z, Ma Z, Yang L, Liu F. PJ34, a PARP1 inhibitor, promotes endothelial repair in a rabbit model of high fat diet-induced atherosclerosis. Cell Cycle. 2019;18(17):2099-2109.