UPF-1069 (1048371-03-4) is a selective PARP-2 inhibitor (IC50=0.3 μM and ~ 27-fold selective against PARP-1).1,2?Increases apoptosis in hippocampal slices but protects cortical cells in models of post-ischemic brain damage.3?Blocks the interaction between PARP-2 and FOXA1, attenuating androgen receptor-mediated gene expression and inhibiting androgen receptor-positive prostate cancer growth.4
1) Pellicciari?et al.?(2008),?On the way to selective PARP-2 inhibitors. Design, synthesis, and preliminary evaluation of a series of isoquinolinone derivatives; Chem. Med. Chem.,?3?914
2) Thorsell?et al.?(2017),?Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors; J. Med. Chem.,?60?1262
3) Moroni?et al.?(2009),?Selective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage; Br. J. Pharmacol.,?157?854
4) Gui?et al.?(2019),?Selective targeting of PARP-2 inhibits androgen receptor signaling and prostate cancer growth through disruption of FOXA1 function; Proc. Natl. Acad. Sci. USA,?116?14573
