3-Aminobenzamide 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。

INO-1001 is an effective inhibitor of PARP (IC50<50 nM in CHO cells) and a mediator of oxidant-induced myocyte dysfunction during reperfusion.

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]

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]

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.

3544-24-9

C7H8N2O

136.154

INO-1001;PARP-IN-1;3-ABA;3-AB;INO 1001;INO1001

H2O:<1 mgml
Ethanol:26 mg/mL (191 mM)
DMSO:26 mg/mL (191 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years