623578-11-0

KU-0058684 is a potent PARP and DNA-PK inhibitors.

KU-0058684 is a potent PARP inhibitor, with an IC50 of 3.2 nM for PARP-1. KU-0058684 significantly reduces DNA double strand break (DSB) repair[1][2].

PARP-1: 3.2 nM (IC₅₀)

[1] Mitchell J, et al. Poly(ADP-Ribose) polymerase-1 and DNA-dependent protein kinase have equivalent roles in double strand break repair following ionizing radiation. Int J Radiat Oncol Biol Phys. 2009 Dec 1;75(5):1520-7. DOI:10.1016/j.ijrobp.2009.07.1722
[2] McCabe N, et al. BRCA2-deficient CAPAN-1 cells are extremely sensitive to the inhibition of Poly (ADP-Ribose) polymerase: an issue of potency. Cancer Biol Ther. 2005 Sep;4(9):934-6. DOI:10.4161/cbt.4.9.2141