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INO-1001_Molecular_structure_CAS_3544-24-9)
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INO-1001

Catalog No. S1132 Name Selleck Chemicals
CAS Number 3544-24-9 Website http://www.selleckchem.com
M. F. C7H8N2O Telephone (877) 796-6397
M. W. 136.15122 Fax (832) 582-8590
Purity Email sales@selleckchem.com
Storage -20°C Chembase ID: 72529

SYNONYMS

IUPAC name
3-aminobenzamide
IUPAC Traditional name
benzamide, 3-amino-

DATABASE IDS

CAS Number 3544-24-9

PROPERTIES

Target PARP
Salt Data Free Base
Solubility DMSO
Storage Condition -20°C

DETAILS

Description (English)
Research Area
Description Reperfusion injury, Malignant melanoma
Biological Activity
Description INO-1001 is a potent inhibitor of PARP with IC50 of 50 nM and a mediator of oxidant-induced myocyte dysfunction during reperfusion.
Targets PARP
IC50 50 nM [1]
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]
Clinical Trials INO-1001 is currently in Phase II clinical trials in patients with Acute Myocardial Infarction.
Features
Combination Therapy
Description In a mismatch repair (MMR)-deficient xenograft, INO-1001 prior to isolated limb infusion (ILI) significantly increased the efficacy of temozolomide (TMZ) and reduces the increase in tumor volume of advanced extremity malignant melanoma than TMZ-ILI alone. [5]
Protocol
Kinase Assay [1]
PARP enzyme activity 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.
Animal Study [3]
Animal Models Male db/db (Leprdb/db) mice.
Formulation INO-1001 is dissolved in water.
Doses ≤60 mg/kg
Administration Administered via p.o.
References
[1] Brock WA, et al. Cancer Lett. 2004, 205(2), 155-160.
[2] Radovits T, et al. Eur J Pharmacol. 2007, 564(1-3), 158-166.
[3] Szabó C, et al. Diabetes. 2006, 55(11), 3004-3012.
[4] Clark RS, et al. J Neurotrauma. 2007, 24(8), 1399-1405.
[5] Toshimitsu H, et al. Ann Surg Oncol. 2010, 17(8), 2247-2254.