PJ34 hydrochloride
(Synonyms: PJ 34 Hydrochloride) 目录号 : GC10145
An inhibitor of poly (ADP-ribose) polymerases
Cas No.:344458-15-7
Sample solution is provided at 25 µL, 10mM.
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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
[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
[2].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
| Cell experiment [1]: | |
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Cell lines |
HepG2 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months. |
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Reaction Conditions |
0.5, 1.0 and 2.0 mg/L; 9 days |
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Applications |
At the doses of 0.5, 1.0 and 2.0 mg/L, PJ34 significantly inhibited HepG2 cell proliferation on days 6 and 9 of culture. |
| Animal experiment [1]: | |
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Animal models |
Nude mice bearing HepG2-derived tumors |
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Dosage form |
3 mg/kg; i.p.; every other day for 21 days |
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Applications |
PJ34 inhibited HepG2 cell-derived tumor growth in nude mice. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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 |
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| Cas No. | 344458-15-7 | SDF | |
| 别名 | PJ 34 Hydrochloride | ||
| 化学名 | 2-(dimethylamino)-N-(6-oxo-5H-phenanthridin-2-yl)acetamide;hydrochloride | ||
| Canonical SMILES | CN(C)CC(=O)NC1=CC2=C(C=C1)NC(=O)C3=CC=CC=C32.Cl | ||
| 分子式 | C17H17N3O2.HCl | 分子量 | 331.8 |
| 溶解度 | ≥ 16.6 mg/mL in DMSO;Water:50 mg/mL (150.69 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0139 mL | 15.0693 mL | 30.1386 mL |
| 5 mM | 0.6028 mL | 3.0139 mL | 6.0277 mL |
| 10 mM | 0.3014 mL | 1.5069 mL | 3.0139 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet