化合物INO1001 T6329

Product Introduction
Bioactivity


英文名: 3-Aminobenzamide

描述: 3-Aminobenzamide (PARP-IN-1) 是一种有效的 PARP 抑制剂，在 CHO 细胞中，对 PARP 的 IC50值约为 50 nM。它是再灌注过程中氧化剂诱导的肌细胞功能障碍的介质。

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

溶解度: Ethanol : 26 mg/mL (191 mM)
DMSO : 55 mg/mL (403.97 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: PARP | inhibit | 3Aminobenzamide | poly ADP ribose polymerase | Inhibitor | 3-Aminobenzamide | 3 Aminobenzamide

相关产品: 5-AIQ | PARP7-IN-16 | Myristicin | Fucosterol | Rucaparib Phosphate | Ru3 | YCH1899 | Niraparib hydrochloride | TNKS-2-IN-1 | Pamiparib

相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Epigenetics Compound Library | Anti-Cancer Active Compound Library | DNA Damage & Repair Compound Library | Apoptosis Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途