5-(2-Oxo-2-phenylethoxy)-3,4-dihydroisoquinolin-1(2H)-one

UPF-1069 (1048371-03-4) is a selective PARP-2 inhibitor (IC50=0.3 μM and ~ 27-fold selective against PARP-1).1,2Increases apoptosis in hippocampal slices but protects cortical cells in models of post-ischemic brain damage.3Blocks the interaction between PARP-2 and FOXA1, attenuating androgen receptor-mediated gene expression and inhibiting androgen receptor-positive prostate cancer growth.4

UPF 1069, is a Selective PARP-2 inhibitor.

PARP-2: 0.3 μM (IC₅₀); PARP-1: 8 μM (IC₅₀)

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[2] ANN-GERD THORSELL. Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors[J]. Journal of Medicinal Chemistry, 2016, 60 4: 1262-1271. DOI:10.1021/acs.jmedchem.6b00990
[3] F MORONI. Selective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage[J]. British Journal of Pharmacology, 2009, 157 5: 854-862. DOI:10.1111/j.1476-5381.2009.00232.x
[4] BIN GUI. Selective targeting of PARP-2 inhibits androgen receptor signaling and prostate cancer growth through disruption of FOXA1 function.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2019: 14573-14582. DOI:10.1073/pnas.1908547116