For research use only. Not for therapeutic Use.
PD-128763 is a selective inhibitor of poly(ADP-ribose) polymerase. PD-128763 has an IC50 value against the purified enzyme approximately 50X lower than 3-aminobenzamide (3-AB), a widely used specific inhibitor of the enzyme. Exposure of exponentially growing cells to a noncytotoxic concentration (0.5 mM) of PD 128763 for 2 h immediately following X irradiation increased their radiation sensitivity, modifying both the shoulder and the slope of the survival curve. When recovery from sublethal damage and potentially lethal damage was examined in exponential and plateau-phase cells, respectively, postirradiation incubation with 0.5 mM PD 128763 was found not only to inhibit both these processes fully, but also to enhance further the level of radiation-induced cell killing. This is in contrast to the slight effect seen with the less potent inhibitor, 3-AB. The results presented suggest that the mechanism of radiosensitization by PD 128763 is related to the potent inhibition of poly(ADP-ribose) polymerase by this compound.( Radiat Res. 1991 Jun;126(3):367-71. ).
| Catalog Number | M110791 |
| CAS Number | 129075-56-5 |
| Molecular Formula | C10H11NO |
| Purity | ≥95% |
| Target | PARP inhibitor |
| Storage | -20°C |
| IUPAC Name | 5-methyl-3,4-dihydro-2H-isoquinolin-1-one |
| InChI | InChI=1S/C10H11NO/c1-7-3-2-4-9-8(7)5-6-11-10(9)12/h2-4H,5-6H2,1H3,(H,11,12) |
| InChIKey | RLLZPXDJYADIEU-UHFFFAOYSA-N |
| SMILES | CC1=CC=CC2=C1CCNC2=O |
| Reference | </br>1: Yau L, Molnar P, Moon MC, Buhay S, Werner JP, Molnar K, Saward L, Del Rizzo D, Zahradka P. Meta-iodobenzylguanidine, an inhibitor of arginine-dependent mono(ADP-ribosyl)ation, prevents neointimal hyperplasia. J Pharmacol Exp Ther. 2008 Sep;326(3):717-24. doi: 10.1124/jpet.108.137513. Epub 2008 Jun 3. PubMed PMID: 18523160.</br>2: Ye DZ, Tai MH, Linning KD, Szabo C, Olson LK. MafA expression and insulin promoter activity are induced by nicotinamide and related compounds in INS-1 pancreatic beta-cells. Diabetes. 2006 Mar;55(3):742-50. PubMed PMID: 16505238.</br>3: Yau L, Litchie B, Zahradka P. MIBG, an inhibitor of arginine-dependent mono(ADP-ribosyl)ation, prevents differentiation of L6 skeletal myoblasts by inhibiting expression of myogenin and p21(cip1). Exp Cell Res. 2004 Dec 10;301(2):320-30. PubMed PMID: 15530866.</br>4: Calabrese CR, Batey MA, Thomas HD, Durkacz BW, Wang LZ, Kyle S, Skalitzky D, Li J, Zhang C, Boritzki T, Maegley K, Calvert AH, Hostomsky Z, Newell DR, Curtin NJ. Identification of potent nontoxic poly(ADP-Ribose) polymerase-1 inhibitors: chemopotentiation and pharmacological studies. Clin Cancer Res. 2003 Jul;9(7):2711-8. PubMed PMID: 12855651.</br>5: Burkart V, Blaeser K, Kolb H. Potent beta-cell protection in vitro by an isoquinolinone-derived PARP inhibitor. Horm Metab Res. 1999 Dec;31(12):641-4. PubMed PMID: 10668915.</br>6: Liu L, Taverna P, Whitacre CM, Chatterjee S, Gerson SL. Pharmacologic disruption of base excision repair sensitizes mismatch repair-deficient and -proficient colon cancer cells to methylating agents. Clin Cancer Res. 1999 Oct;5(10):2908-17. PubMed PMID: 10537360.</br>7: Yau L, Elliot T, Lalonde C, Zahradka P. Repression of phosphoenolpyruvate carboxykinase gene activity by insulin is blocked by 3-aminobenzamide but not by PD128763, a selective inhibitor of poly(ADP-ribose) polymerase. Eur J Biochem. 1998 Apr 1;253(1):91-100. PubMed PMID: 9578465.</br>8: Chatterjee S, Cheng MF, Berger RB, Berger SJ, Berger NA. Effect of inhibitors of poly(ADP-ribose) polymerase on the induction of GRP78 and subsequent development of resistance to etoposide. Cancer Res. 1995 Feb 15;55(4):868-73. PubMed PMID: 7850801.</br> |
