| 名稱(chēng) | PJ34 hydrochloride |
| 描述 | PJ34 hydrochloride (PJ34 HCl) is a potent specific inhibitor of PARPl/2. |
| 細(xì)胞實(shí)驗(yàn) | 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. |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 在MBP免疫的PLSJL小鼠中,PJ34部分抑制脊髓組織中TNF-α和ICAM-1的表達(dá),抑制EAE的臨床體征的發(fā)展.在全身性?xún)?nèi)毒素血癥模型中,PJ34能夠減低血漿TNF-α,IL-1β和亞硝酸鹽/硝酸鹽的含量. 在非肥胖糖尿病小鼠中,強(qiáng)飼口服PJ34能夠抑制硫酸葡聚糖結(jié)腸炎反應(yīng). |
| 體內(nèi)活性 | 在過(guò)氧亞硝酸鹽誘導(dǎo)的細(xì)胞中（EC 50=20 nM）,PJ34能夠抑制細(xì)胞壞死的發(fā)生。 |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 41.67 mg/mL (125.59 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (3.01 mM), Sonication is recommended.
H2O : 33.2 mg/mL (100.06 mM), Sonication is recommended.
|
| 關(guān)鍵字 | poly ADP ribose polymerase | PJ-34 Hydrochloride | PJ34 hydrochloride | PJ-34 | PJ34 | PJ 34 Hydrochloride | PJ 34 | PARP | Inhibitor | inhibit |
| 相關(guān)產(chǎn)品 | Taurodeoxycholate sodium salt | Niraparib | XAV-939 | Olaparib | 3-Aminobenzamide | Benzamide | Niraparib tosylate monohyrate | AZ9482 | OUL35 | RMC-7977 | BGP-15 | 7-Methylguanine |
| 相關(guān)庫(kù) | 抑制劑庫(kù) | 抗乳腺癌化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 抗癌化合物庫(kù) | 已知活性化合物庫(kù) | 抗衰老化合物庫(kù) | 表觀遺傳庫(kù) | NO PAINS 化合物庫(kù) | 抗卵巢癌化合物庫(kù) | DNA 損傷和修復(fù)分子庫(kù) | 免疫/炎癥分子化合物庫(kù) | 抗前列腺癌化合物庫(kù) |