PJ34 hydrochloride是一种有效且特异性的PARP抑制剂，IC50值为110nM。
Cas No.:344458-15-7
Sample solution is provided at 25 µL, 10mM.
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PJ34 hydrochloride is an effective and specific PARP inhibitor with an IC50 value of 110nM [1]. PJ34 hydrochloride promotes cell death by inhibiting PARP1-mediated DNA repair, and leads to a decrease in NF-κB expression and specifically blocks the mitosis of cancer cells[2]. PJ34 hydrochloride has been widely used to kill tumor cells and has been employed in the development of novel combined therapies to efficiently enhance the cytotoxicity of chemotherapy drugs[3].
In vitro, PJ34 hydrochloride treatment for 48 hours significantly inhibited the viability of OVCAR-3 cells and SKOV-3 cells, with the IC50 values being 18.7µM and 28.5µM, respectively[4]. Treatment with 50µM PJ34 hydrochloride for 72 hours induced cell cycle arrest and apoptosis in HTLV-I-transformed MT-2 cells[5]. Treatment with 10µM PJ34 hydrochloride for 24 hours resulted in mitotic defects in M14 cells and promoted abnormal accumulation of actin in the nucleolus[6].
In vivo, PJ34 hydrochloride treatment via intraperitoneal injection at a dose of 10mg/kg three times weekly for 4 weeks alleviated the accumulation of triglycerides (TG) in the liver of alcohol-fed mice and reduced the hepatic gene expression of sterol regulatory element-binding protein 1c, DGAT1, and DGAT2[7]. Intraperitoneal injection of PJ34 hydrochloride (50μg) at 2 hours before and 6 hours after middle cerebral artery occlusion (MCAo) significantly reduced the cerebral infarct volume in SV/129 mice [8].
References:
[1] Iwashita A, Tojo N, Matsuura S, et al. A novel and potent poly (ADP-ribose) polymerase-1 inhibitor, FR247304 (5-chloro-2-[3-(4-phenyl-3, 6-dihydro-1 (2 H)-pyridinyl) propyl]-4 (3 H)-quinazolinone), attenuates neuronal damage in in vitro and in vivo models of cerebral ischemia[J]. The Journal of pharmacology and experimental therapeutics, 2004, 310(2): 425-436.
[2] Cohen-Armon M. The modified phenanthridine PJ34 unveils an exclusive cell-death mechanism in human cancer cells[J]. Cancers, 2020, 12(6): 1628.
[3] Mann M, Chauhan S S, Kumar S, et al. PJ34-mediated PARP-1 enzymatic activity inhibition in cervical cancer modulates the cellular response to cisplatin[J]. Cancer Research, 2016, 76(14_Supplement): 2152-2152.
[4] Güler A E, Tuncer M C, Özdemir İ. Synergistic Antitumor Activity of Curcumin and the PARP1 Inhibitor PJ34 in Platinum-Sensitive and Resistant Ovarian Cancer Cells[J]. Cancers, 2026, 18(4): 620.
[5] Bai X T, Moles R, Chaib-Mezrag H, et al. Small PARP inhibitor PJ-34 induces cell cycle arrest and apoptosis of adult T-cell leukemia cells[J]. Journal of hematology & oncology, 2015, 8(1): 117.
[6] Chevanne M, Zampieri M, Caldini R, et al. Inhibition of PARP activity by PJ‐34 leads to growth impairment and cell death associated with aberrant mitotic pattern and nucleolar actin accumulation in M14 melanoma cell line[J]. Journal of cellular physiology, 2010, 222(2): 401-410.
[7] Huang S, Zhang B, Chen Y, et al. Poly (ADP-ribose) polymerase inhibitor PJ34 attenuated hepatic triglyceride accumulation in alcoholic fatty liver disease in mice[J]. The Journal of pharmacology and experimental therapeutics, 2018, 364(3): 452-461.
[8] Abdelkarim G E, Gertz K, Harms C, et al. Protective effects of PJ34, a novel, potent inhibitor of poly (ADP-ribose) polymerase (PARP) in in vitro and in vivo models of stroke[J]. International journal of molecular medicine, 2001, 7(3): 255-260.
PJ34 hydrochloride是一种有效且特异性的PARP抑制剂，IC50值为110nM[1]。PJ34 hydrochloride通过抑制PARP1介导的DNA修复来促进细胞死亡，导致NF-κB表达降低，并能特异性地阻断癌细胞的有丝分裂[2]。PJ34 hydrochloride已被广泛用于杀灭肿瘤细胞，并已被用于开发新型联合疗法，以有效增强化疗药物的细胞毒性[3]。
在体外，PJ34 hydrochloride处理OVCAR-3细胞和SKOV-3细胞48小时，显著抑制了细胞活力，IC50值分别为18.7µM和28.5µM[4]。50µM的PJ34 hydrochloride处理HTLV-I转化的MT-2细胞72小时，诱导了细胞周期阻滞和凋亡[5]。10µM的PJ34 hydrochloride处理M14细胞24小时，导致有丝分裂缺陷，并促进了肌动蛋白在核仁中的异常积累[6]。
在体内，每周腹腔注射3次10mg/kg剂量的PJ34 hydrochloride，持续4周，减轻了酒精喂养小鼠肝脏中的甘油三酯（TG）积累，并降低了肝脏中sterol regulatory element-binding protein 1c、DGAT1和DGAT2的基因表达[7]。在脑中动脉闭塞前2小时和后6小时分别腹腔注射50µg的PJ34 hydrochloride，显著减少了SV/129小鼠的脑梗死体积[7]。
| Cell experiment [1]: | |
Cell lines | OVCAR-3 cells |
Preparation Method | OVCAR-3 cells were grown in RPMI-1640 medium with 10% (v/v) fetal bovine serum (FBS), antibiotic/antimycotic solution at 37°C in 5% CO2/atmosphere. Cells were seeded in 96-well plates at a density of 5×103 cells and cultured overnight. After 48h of treatment with different concentrations of PJ34 hydrochloride (0, 5, 10, 25, 50, and 100µM), the cell viability was measured. |
Reaction Conditions | 0, 5, 10, 25, 50, and 100µM; 48h |
Applications | PJ34 hydrochloride treatment significantly inhibited the cell viability of OVCAR-3 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6 mice |
Preparation Method | Male C57BL/6 mice (8 weeks old; 21-23g) were housed singly in a standard environment with food and water ad libitum. All mice were fed for 4 weeks with liquid diets. The pair-fed diet (PF) contained 18% protein, 35% fat, and 47% carbohydrate, whereas the alcohol-fed diet (AF) contained 18% protein, 35% fat, 11% carbohydrate, and 36% alcohol. PJ34 hydrochloride (10mg/kg) was injected intraperitoneally three times a week for 4 weeks. The same volume of physiologic saline (0.1ml/20g per day; i.p.) was injected intraperitoneally three times a week as a vehicle treatment. At the end of the experiment, liver samples were harvested for analysis. |
Dosage form | 10mg/kg; three times a week for 4 weeks; i.p. |
Applications | PJ34 hydrochloride treatment significantly reduced the accumulation of TG in the liver of alcohol-fed mice. |
References: | |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0139 mL | 15.0693 mL | 30.1386 mL |
| 5 mM | 602.8 μL | 3.0139 mL | 6.0277 mL |
| 10 mM | 301.4 μL | 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，
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2.
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- Purity: >99.00% Appearance: A solid
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