Description
NU 1025 is an inhibitor of poly(ADP-
ribose) polymerases (PARP) (IC
50 = 400 nM). It enhances the cytotoxicity of γ-
irradiation and certain anticancer drugs. NU 1025 is also used to study the regulation of deoxyribonucleic acid repair by PARP enzymes.
Chemical Properties
Off-White to Pale Yellow Solid
Uses
A potent inhibitor of poly (ADP-ribose) polymerase (PARP). Ki and IC50 values are 48 and 400 nM respectively.
Uses
NU 1025 is an inhibitor of poly(ADP-ribose) polymerases (PARP) (IC50 = 400 nM). It enhances the cytotoxicity of γ-irradiation and certain anticancer drugs. NU 1025 is also used to study the regulation of deoxyribonucleic acid repair by PARP enzymes.[Cayman Chemical]
Definition
ChEBI: A member of the class of quinazolines that is quinazolin-4(1H)-one substituted by a hydroxy group at position 8 and a methyl group at position 2. It has been shown to exhibit inhibitory activity against poly(ADP-ribose) polymerase.
Biological Activity
Novel, potent inhibitor of poly(ADP-ribose) polymerase (PARP). K i and IC 50 values are 48 and 400 nM respectively.
References
[1] ROGER J. GRIFFIN. Resistance-Modifying Agents. 5. 1 Synthesis and Biological Properties of Quinazolinone Inhibitors of the DNA Repair Enzyme Poly(ADP-ribose) Polymerase (PARP)[J]. Journal of Medicinal Chemistry, 1998, 41 26: 5247-5256. DOI:
10.1021/jm980273t[2] KJ BOWMAN. Potentiation of anti-cancer agent cytotoxicity by the potent poly(ADP-ribose) polymerase inhibitors NU1025 and NU1064[J]. British Journal of Cancer, 1998, 78 10: 1269-1277. DOI:
10.1038/bjc.1998.670[3] C A DELANEY. Potentiation of temozolomide and topotecan growth inhibition and cytotoxicity by novel poly(adenosine diphosphoribose) polymerase inhibitors in a panel of human tumor cell lines.[J]. Clinical Cancer Research, 2000, 6 7: 2860-2867.
[4] SLAWOMIR KUMALA. Repair of DNA strand breaks in a minichromosome in vivo: kinetics, modeling, and effects of inhibitors.[J]. PLoS ONE, 2013: e52966. DOI:
10.1371/journal.pone.0052966
