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INO-1001

In stock
Catalog No.
A4161
Potent PARP inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$55.00
In stock
250mg
$70.00
In stock
500mg
$110.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt136.15
Cas No.3544-24-9
FormulaC7H8N2O
Synonyms3-aminobenzamide
Solubility≥7.35 mg/mL in DMSO, ≥48.1 mg/mL in EtOH with ultrasonic, ≥23.45 mg/mL in H2O with ultrasonic
Chemical Name3-aminobenzamide
SDFDownload SDF
Canonical SMILESC1=CC(=CC(=C1)N)C(=O)N
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

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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