PJ34 HCl | PARP Inhibitor | AmBeed-信号通路专用抑制剂

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PJ34 盐酸 /PJ34 HCl {[allProObj[0].p_purity_real_show]}

货号：A103485 同义名： PJ-34 (hydrochloride);PJ34 hydrochloride

PJ34 HCl是一种 PARP1/2 抑制剂，IC50 值分别为 110 nM 和 86 nM。

PJ34 HCl 化学结构
CAS号：344458-15-7

PJ34 HCl 3D分子结构
CAS号：344458-15-7

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PJ34 HCl 纯度/质量文件产品仅供科研

货号：A103485 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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PARP 亚型比较

产品名称	PARP ↓ ↑	PARP1 ↓ ↑	PARP2 ↓ ↑	PARP3 ↓ ↑	纯度
PJ34 HCl	++ PARP, EC50: 20 nM				99%+
Rucaparib phosphate	++++ PARP, Ki: 1.4 nM				99%+
3-Aminobenzamide	++ PARP, IC50: <50 nM				98%
AZD-2461	✔				99%+
BGP-15	✔				99%+
NU1025	+ PARP, IC50: 400 nM				97%
Benzamide	+ PARP, IC50: 3.3 μM				98%
Picolinamide	+ PARP, IC50: 95 μM				98%
AG14361		+++ PARP1, Ki: <5 nM			98+%
Iniparib		✔			98%
Talazoparib		++++ PARP1, IC50: 0.57 nM			99%+
NMS-P118		++ PARP1, Kd: 0.009 μM			98+%
UPF 1069		+ PARP1, IC50: 8.0 μM	++ PARP2, IC50: 0.3 μM		98%
A-966492		++++ PARP1, Ki: 1 nM PARP1, EC50: 1 nM	+++ PARP2, Ki: 1.5 nM		99%+
Veliparib		++ PARP1, Ki: 5.2 nM	+++ PARP2, Ki: 2.9 nM		98%
Niraparib tosylate		+++ PARP1, IC50: 3.8 nM	+++ PARP2, IC50: 2.1 nM		99%+
Stenoparib		++++ PARP1, IC50: 1 nM	++++ PARP2, IC50: 1.2 nM		98%
Olaparib		+++ PARP1, IC50: 5 nM	++++ PARP2, IC50: 1 nM		98%
Niraparib		+++ PARP1, IC50: 3.8 nM	+++ PARP2, IC50: 2.1 nM		98%
ME0328		+ PARP1, IC50: 6.3 μM		+ PARP3, IC50: 0.89 μM	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

PJ34 HCl 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].

PJ34 HCl 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
MEF cells		Proliferation assay	72 h	Antiproliferative activity against MEF cells harboring Brca1 deletion mutant at exon 11 assessed as cell viability after 72 hrs by MTT assay, IC50=13.2 μM	22365563

PJ34 HCl 动物研究

Dose	Rat: 10 mg/kg^[3] (i.v.); 30 mg/kg^[4] (p.o.) Mice: 1.5 mg/kg - 25 mg/kg^[5] (i.p.)
Administration	i.v., p.o., i.p.

PJ34 HCl 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.

PJ34 HCl 实验方案

计算器

存储液制备

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

PJ34 HCl 技术信息

CAS号	344458-15-7
分子式	C₁₇H₁₈ClN₃O₂
分子量	331.797

别名	PJ-34 (hydrochloride);PJ34 hydrochloride
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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

PJ34 盐酸 /PJ34 HCl {[allProObj[0].p_purity_real_show]}

PJ34 HCl 纯度/质量文件产品仅供科研

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PJ34 HCl 质控信息

PJ34 HCl 生物活性

PJ34 HCl 细胞研究

PJ34 HCl 动物研究

PJ34 HCl 参考文献

PJ34 HCl 实验方案

PJ34 HCl 技术信息

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PJ34 盐酸 /PJ34 HCl {[allProObj[0].p_purity_real_show]}

PJ34 HCl 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

PJ34 HCl 质控信息

PJ34 HCl 生物活性

PJ34 HCl 细胞研究

PJ34 HCl 动物研究

PJ34 HCl 参考文献

PJ34 HCl 实验方案

PJ34 HCl 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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PJ34 HCl 纯度/质量文件产品仅供科研