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KI3355INO-1001250 mg$170

Chemical Characteristic

Product NameINO-1001
Synonyms3-Aminobenzamide
CAS No.3544-24-9
Molecular Weight 136.15
FormulaC7H8N2O
Chemical Name3-Aminobenzamide
SmilesC(=O)(c1cc(ccc1)N)N
Chemical Structure

Biological activities

INO-1001 is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. INO-1001 at non-cytotoxic concentrations effectively inhibits PARP activity and potently enhances the radiation sensitivity in human and rodent fibroblast cell lines in vitro.[1] INO-1001 also improves endothelial dysfunction induced by reactive oxidant hydrogen peroxide (H2O2) in vitro.[2] In vitro, INO-1001 blocks the hyperglycemia-induced ROS generation in podocytes and prevents hyperglycemia-induced nuclear factor-ΚB (NF-ΚB) activation of podocytes. In vivo, INO-1001 treatment decreases diabetes-induced podocyte depletion and ameliorates nephropathy of type 2 diabetic Leprdb/db mice.[3] In an animal model of regional therapy for the treatment of advanced extremity malignant melanoma, INO-1001 treatment prior to IL-I significantly enhances the efficacy of temozolomide.[4] Moreover, in an experimental dog model of cardioplegic arrest and extracorporal circulation, INO-1001 administration (1 mg/kg) improves cardiac and pulmonary function.[5]

Protocols

In vivo, INO-1001 is dissolved in 5% dextrose.[6]

References

[1] Brock WA, 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.
[2] Radovits T, et al. Poly(ADP-ribose) polymerase inhibition improves endothelial dysfunction induced by reactive oxidant hydrogen peroxide in vitro. Eur J Pharmacol. 2007, 564(1-3): 158-166.
[3] Szabò C, et al. Poly(ADP-ribose) polymerase inhibitors ameliorate nephropathy of type 2 diabetic Leprdb/db mice. Diabetes. 2006, 55(11): 3004-3012.
[4] Toshimitsu H, et al. Inhibition of poly(ADP-ribose) polymerase enhances the effect of chemotherapy in an animal model of regional therapy for the treatment of advanced extremity malignant melanoma. Ann Surg Oncol. 2010, 17(8): 2247-2254.
[5] Szabò G, 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.
[6] Cheng CL, et al. Poly(ADP-ribose) polymerase-1 inhibition reverses temozolomide resistance in a DNA mismatch repair-deficient malignant glioma xenograft. Mol Cancer Ther. 2005, 4(9): 1364-1368.

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