Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PJ34 hydrochloride (PJ34 HCl) 是一种 PARP1/2的特异性有效抑制剂,IC50值分别为 110 nM 和 86 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
10 mg | ¥ 416 | 现货 | ||
25 mg | ¥ 865 | 现货 | ||
50 mg | ¥ 1,298 | 现货 | ||
100 mg | ¥ 2,318 | 现货 | ||
200 mg | ¥ 2,939 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 461 | 现货 |
产品描述 | PJ34 hydrochloride (PJ34 HCl) is a potent specific inhibitor of PARPl/2. |
靶点活性 | PARP:20 nM(EC50) |
体外活性 | 在MBP免疫的PLSJL小鼠中,PJ34部分抑制脊髓组织中TNF-α和ICAM-1的表达,抑制EAE的临床体征的发展.在全身性内毒素血症模型中,PJ34能够减低血浆TNF-α,IL-1β和亚硝酸盐/硝酸盐的含量. 在非肥胖糖尿病小鼠中,强饲口服PJ34能够抑制硫酸葡聚糖结肠炎反应. |
体内活性 | 在过氧亚硝酸盐诱导的细胞中(EC 50=20 nM),PJ34能够抑制细胞坏死的发生。 |
激酶实验 | To assess the PARP-1 or PARP-2 inhibitory activity of FR247304, 3-AB, and PJ34, PARP activity is evaluated with minor modifications. PARP enzyme assay is carried out in a final volume of 100 μL consisting of 50 mM Tris-HCl (pH 8.0), 25 mM MgCl2, 1 mM dithiothreitol, 10 μg activated salmon sperm DNA, 0.1 μCi of [adenylate-32P]NAD, 0.2 units of recombinant human PARP for PARP-1 assay or 0.1 units of recombinant mouse PARP-2 for PARP-2 assay, and various concentrations of FR261529 or 3-AB. The reaction mixture is incubated at room temperature (23°C) for 15 min, and the reaction is terminated by adding 200 μL of ice-cold 20% trichloroacetic acid (TCA) and incubated at 4°C for 10 min. The precipitate is transferred onto GF/B filter and washed three times with 10% TCA solution and 70% ethanol. After the filter is dried, the radioactivity is determined by liquid scintillation counting. |
细胞实验 | PJ34 is dissolved in 100% DMSO at 10 mM and then diluted in DMEM without serum[1]. PC12 cell cultured are grown in Dulbecco's modified Eagle's medium supplemented with 5% (v/v) fetal calf serum, 5% (v/v) horse serum, and a 1% (v/v) penicillin-streptomycin antibiotics mixture. Cells are grown in an atmosphere of 95% air and 5% CO2 at 37°C. For all experiment, cells are seeded at a density of 4×104 cells/well in 96-well culture plates and allowed to attach overnight. For assessment of cell viability, hydrogen peroxide-induced cytotoxicity is quantified by a standard measurement of LDH release with the use of the LDH assay kit. Briefly, 6 h after hydrogen peroxide exposure, 20 μL of medium of each well is collected, and the solution prepared from LDH assay kit is added. After incubation at room temperature for 30 min, the reaction is stopped by addition of 1 N HCl, and absorbance is measured at 450 nm using a microplate reader. |
别名 | PJ34 HCl |
分子量 | 331.8 |
分子式 | C17H18ClN3O2 |
CAS No. | 344458-15-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 33.2 mg/mL (100 mM)
H2O: 33.2 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O | 1 mM | 3.0139 mL | 15.0693 mL | 30.1386 mL | 75.3466 mL |
5 mM | 0.6028 mL | 3.0139 mL | 6.0277 mL | 15.0693 mL | |
10 mM | 0.3014 mL | 1.5069 mL | 3.0139 mL | 7.5347 mL | |
20 mM | 0.1507 mL | 0.7535 mL | 1.5069 mL | 3.7673 mL | |
50 mM | 0.0603 mL | 0.3014 mL | 0.6028 mL | 1.5069 mL | |
100 mM | 0.0301 mL | 0.1507 mL | 0.3014 mL | 0.7535 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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