INO-1001 (3-Aminobenzamide)

Catalog No.S1132 Synonyms: 3-ABA , 3-amino Benzamide, 3-AB

INO-1001 (3-Aminobenzamide) Chemical Structure

Molecular Weight(MW): 136.15

INO-1001 is a potent inhibitor of PARP with IC50 of <50 nM in CHO cells and a mediator of oxidant-induced myocyte dysfunction during reperfusion. Phase 2.

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2 Customer Reviews

  • Propofol inhibited the increase of PARP-1׳s expression and activity. Mice (n=6) were injected intraperitoneally with propofol, INO-1001 (a PARP-1 inhibitor) or equal volume of normal saline (NS), and then were trained with objects. Naïve animals were injected with normal saline and trained without objects (the same as habituation). 30 min after acquisition trial, the hippocampal tissues were harvested for determining PARP-1 (A and B) and PAR (C and D) expression by Western blot. Histogram represented the relative level normalized to naïve. *P<0.05, **P<0.01.

    Brain Res, 2016, 1637:137-45. . INO-1001 (3-Aminobenzamide) purchased from Selleck.

    Effect of DPQ and INO-1001 on ADP-, collagen- or PAR1ap-induced platelet aggregation. Human PRP samples were preincubated with PARP inhibitor (50 μM) or its vehicle and then stimulated with ADP (1.5 to 5 μM; to produce a biphasic aggregation curve), collagen (1 to 2 μg/ml) or PAR1ap (1 to 2 μM). Results are expressed relatively to platelet agonist alone (=vehicle group; normalized to 100%) and presented as the mean±SD (n=5-6).

    PLoS One, 2014, 9(10):e110776.. INO-1001 (3-Aminobenzamide) purchased from Selleck.

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Biological Activity

Description INO-1001 is a potent inhibitor of PARP with IC50 of <50 nM in CHO cells and a mediator of oxidant-induced myocyte dysfunction during reperfusion. Phase 2.
Targets
PARP [1]
<50 nM
In vitro

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 H2O2. [2]

In vivo 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]

Protocol

Animal Research:[3]
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  • Animal Models: Male db/db (Leprdb/db) mice.
  • Formulation: INO-1001 is dissolved in water.
  • Dosages: ≤60 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 27 mg/mL (198.31 mM)
Ethanol 27 mg/mL (198.31 mM)
Water Insoluble
In vivo Add solvents individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 136.15
Formula

C7H8N2O

CAS No. 3544-24-9
Storage powder
Synonyms 3-ABA , 3-amino Benzamide, 3-AB

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00271167 Terminated Heart Diseases|Postoperative Complications Inotek Pharmaceuticals Corporation October 2005 Phase 2
NCT00272415 Terminated Melanoma Genentech, Inc. October 2005 Phase 1
NCT00271765 Completed Acute Myocardial Infarction Inotek Pharmaceuticals Corporation January 2004 Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Related Antibodies

PARP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID