1825345-33-2

AZ9482 is a poly(ADP-ribose) polymerase (PARP) inhibitor (IC₅₀s = 1, 1, 46, 640, 9, and 160 nM for PARP1, -2, -3, -6, TNKS1/PARP5a, and TNKS2, respectively). It induces centrosome declustering (EC₅₀ = <18 nM) and a multipolar spindle phenotype in HeLa cells. AZ9482 inhibits the growth of OCI-LY19 diffuse large B cell lymphoma (DLBCL) cells (GI₅₀ = 3 nM).

AZ9482 is a triple PARP1/2/6 inhibitor, with IC50 values of 1 nM, 1 nM and 640 nM for PARP1, PARP2 and PARP6, respectively[1].

[1] Ryan T Howard, et al. Structure-Guided Design and In-Cell Target Profiling of a Cell-Active Target Engagement Probe for PARP Inhibitors. ACS Chem Biol. 2020 Feb 21;15(2):325-333. DOI:10.1021/acschembio.9b00963