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INO-1001Potent PARP inhibitor

INO-1001

Catalog No. A4161
Size Price Stock Qty
10mM (in 1mL DMSO) $55.00 In stock
250mg $70.00 In stock
500mg $110.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

INO-1001

Biological Activity

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          
IC50 50 nM          

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Chemical Properties

Cas No. 3544-24-9 SDF Download SDF
Synonyms 3-aminobenzamide
Chemical Name 3-aminobenzamide
Canonical SMILES C1=CC(=CC(=C1)N)C(=O)N
Formula C7H8N2O M.Wt 136.15
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

INO-1001 is a potent and selective inhibitor of PARP [1].

Poly(ADP-ribose) polymerase (PARP) is an enzyme involved in DNA repair and as a mediator of energy failure-induced cell death and NAD+ depletion [1].

In rodent and human fibroblast cell lines, INO-1001 significantly inhibited PARP activity. Treatment of 10 μM INO-1001 and a single dose of radiation caused significant radiosensitization of the three cells lines. While apoptosis was not increased, suggesting that INO-1001 increased radiation-induced cell killing through interfering with DNA repair mechanisms, increasing necrotic cell death [2].

In adult male mice subjected to moderate controlled cortical impact (CCI), injection intracerebral with INO-1001 (1.6 mg/kg) preserved brain NAD+ levels. In the Morris water maze, INO-1001 reduced the latency time to find the hidden platform and increased the time in the target quadrant [1]. In dogs underwent hypothermic cardiopulmonary bypass, reperfusion for 60 min after treatment with INO-1001 (1 mg/kg), INO-1001 significantly recovered left and right ventricular systolic function, increased coronary blood flow [3].

References:

[1]. Clark RS, Vagni VA, Nathaniel PD, et al. Local administration of the poly(ADP-ribose) polymerase inhibitor INO-1001 prevents NAD+ depletion and improves water maze performance after traumatic brain injury in mice. J Neurotrauma, 2007, 24(8): 1399-1405.

[2]. Szabó G, Soós P, Mandera S, et al. INO-1001 a novel poly(ADP-ribose) polymerase (PARP) inhibitor improves cardiac and pulmonary function after crystalloid cardioplegia and extracorporal circulation. Shock, 2004, 21(5): 426-432.

[3]. Brock WA, Milas L, Bergh S, et al. Radiosensitization of human and rodent cell lines by INO-1001, a novel inhibitor of poly(ADP-ribose) polymerase. Cancer Lett, 2004, 205(2): 155-160.