名称 | 3-Aminobenzamide |
描述 | 3-Aminobenzamide (PARP-IN-1) is a potent PARP inhibitor (IC50 < 50 nM in CHO cells) and mediates oxidant-induced myocyte dysfunction during reperfusion. |
激酶实验 | PARP activity is measured with a PARP Activity Assay Kit. This method measures relative PARP activity by determining the level of incorporation of?3H-NAD into trichloroacetic acid (TCA) precipitable material in the presence of sheared genomic DNA, which activates PARP. The reaction mixture is added directly to washed cultures in 12-well culture plates and the reaction is allowed to proceed for 60 minutes at 37°C before the cells are removed mechanically, transferred to a microcentrifuge tube, and precipitated with ice-cold 5% TCA. |
体外活性 | INO-1001 (>1 μM) leads to more than 95% inhibition of PARP activity without significant cellular toxicity. In addition, INO-1001 significantly sensitizes CHO cells by blocking most of the DNA repair occurring between radiation fractions. [1] Inhibition of PARP activity by INO-1001 significantly improves endothelial function by enhancing the acetylcholine-induced, endothelium-dependent, nitric oxide mediated vasorelaxation after exposure with 400 μM Water2. [2] |
体内活性 | In a db/db (Leprdb/db) mouse model, INO-1001 ameliorates diabetes-induced albumin excretion and mesangial expansion, and also decreases diabetes-induced podocyte depletion. [3] Treatment with INO-1001 (1.6 mg/kg via intracerebral injection) prevents NAD+ depletion and improves water maze performance after controlled cortical impact (CCI) in mice. [4] |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | Ethanol : 26 mg/mL (191 mM) DMSO : 55 mg/mL (403.97 mM) H2O : < 1 mg/mL (insoluble or slightly soluble)
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关键字 | PARP | inhibit | 3Aminobenzamide | poly ADP ribose polymerase | Inhibitor | 3-Aminobenzamide | 3 Aminobenzamide |
相关产品 | 4'-Methoxychalcone | Niraparib tosylate monohyrate | VPC-70063 | XAV-939 | Niraparib | 3-Methoxybenzamide | Talazoparib | NU1025 | Olaparib | Benzamide | Picolinamide | OUL35 |
相关库 | 经典已知活性库 | 抗乳腺癌化合物库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 抑制剂库 | 抗衰老化合物库 | 临床期小分子药物库 | 已知活性化合物库 | 抗癌活性化合物库 | 抗癌药物库 |