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PJ34 hydrochloride

现货
Catalog No.
A4159
有效的细胞渗透性PARP抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 650.00
现货
5mg
¥ 500.00
现货
10mg
¥ 600.00
现货
50mg
¥ 1,700.00
现货

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Background

PJ34 is a novel and potent inhibitor of poly(ADP-ribose) polymerase (PARP), an enzyme involved in DNA repair and cell proliferation, that dose-dependently inhibits purified PARP enzyme in a cell-free assay with half maximal effective concentration EC50 value of 20 nM. Unlike other PARP inhibitors (such as 3-AB), PJ34 does not possess any antioxidant properties but exhibits 10,000 times greater PARP inhibition than 3-AB (EC50 = 200 μM). PJ34 has been found to have neuro-protective effects and enhance the chemotherapeutic effects in several tumor types. Study results have shown that PJ34 inhibits peroxynitrite-induced cell necrosis with EC50 value of 20 nM and dose-dependently suppresses the growth of HepG2 cells.

Reference

Sheng-Hui Huang, Min Xiong, Xiao-Ping Chen, Zhen-Yu Xiao, Yin-Feng Zhao and Zhi-Yong Huang. PJ34, an inhibitor of PARP-1, suppresses cell growth and enhances the suppressive effects of cisplatin in liver cancer cells. Oncology Reports 20: 567-572, 2008

Galaleldin E. Abdelkarim, Karen Gertz, Christoph Harms, Juri Katchanov, Ulrich Dirnagl, Csaba Szabo and Matthias Enders. Protective effects of PJ34, a novel, potent inhibitor of poly(ADP-ribose) polymerase (PARP) in in vitro and in vivo models of stroke. International Journal of Molecular Medicine 7: 255-260, 2001

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt331.8
Cas No.344458-15-7
FormulaC17H17N3O2.HCl
SynonymsPJ 34 Hydrochloride
Solubility≥16.6 mg/mL in DMSO, <2.5 mg/mL in EtOH, <2.47 mg/mL in H2O
Chemical Name2-(dimethylamino)-N-(6-oxo-5H-phenanthridin-2-yl)acetamide;hydrochloride
SDFDownload SDF
Canonical SMILESCN(C)CC(=O)NC1=CC2=C(C=C1)NC(=O)C3=CC=CC=C32.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

HepG2细胞

制备方法

在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

0.5、1.0和2.0 mg/L;9天

实验结果

在0.5、1.0和2.0 mg/L的剂量下,PJ34于培养后的第6和9天显著抑制HepG2细胞增殖。

动物实验 [1]:

动物模型

携带HepG2肿瘤的裸鼠

给药剂量

3 mg/kg;腹腔注射;隔天给药,持续21天

实验结果

在裸鼠中,PJ34抑制HepG2肿瘤生长。

其它注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Sheng-Hui Huang, Min Xiong, Xiao-Ping Chen, Zhen-Yu Xiao, Yin-Feng Zhao and Zhi-Yong Huang. PJ34, an inhibitor of PARP-1, suppresses cell growth and enhances the suppressive effects of cisplatin in liver cancer cells. Oncology Reports 20: 567-572, 2008

生物活性

PJ34是一种新型有效的PARP-l/2特异性抑制剂,其EC50值为20 nM。.
靶点 PARP          
IC50 20 nM (EC50)          

质量控制

化学结构

PJ34 hydrochloride

相关生物数据

PJ34 hydrochloride

相关生物数据

PJ34 hydrochloride