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PJ34 盐酸 /PJ34 HCl 99%+

货号:A103485 同义名: PJ-34 (hydrochloride);PJ34 hydrochloride Ambeed 开学季,买赠积分,赢豪礼

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 化学结构
CAS号:344458-15-7
PJ34 HCl 3D分子结构
CAS号:344458-15-7
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: 99%+
批次查询: 批次纯度:

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产品名称 PARP PARP1 PARP2 PARP3 其他靶点 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, EC50: 1 nM

PARP1, Ki: 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

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

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