UPF-1069
PARP-2 inhibitor / 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
Biochemicals & reagents
1048371-03-4
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
-20°C
TARGET: PARP; Kinase -- PATHWAY: Transcription; DNA repair -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer; Ischemia