Drug intelligence / Profile preview

NU1025

Development stage
Preclinical
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
01

Overview

NU1025 is a potent small molecule inhibitor of poly(ADP-ribose) polymerase 1 (PARP-1), with an IC50 of approximately 400 nM. It belongs to the quinazoline class of organic compounds and has the chemical formula C9H8N2O2. NU1025 enhances the cytotoxicity of DNA-damaging agents such as ionizing radiation and various anticancer drugs, including temozolomide, topotecan, bleomycin, and MTIC. Preclinical studies have demonstrated its anti-cancer activity as well as neuroprotective effects in models of cerebral ischemia by reducing NAD depletion and DNA fragmentation through inhibition of PARP-mediated cell death pathways[1][3][5][7][8]. NU1025 was initially developed for research purposes and has not been approved for clinical use.

Other names
8-hydroxy-2-methylquinazoline-4-onePARP Inhibitor VINSC 696807NSC696807NSC-696807
02

Targets

PARP1 (Poly (adp-ribose) polymerase 1)

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