5-(2-Oxo-2-phenylethoxy)-3,4-dihydroisoquinolin-1(2H)-one
5-(2-Oxo-2-phenylethoxy)-3,4-dihydroisoquinolin-1(2H)-one Basic information
- Product Name:
- 5-(2-Oxo-2-phenylethoxy)-3,4-dihydroisoquinolin-1(2H)-one
- Synonyms:
-
- 5-(2-Oxo-2-phenylethoxy)-3,4-dihydroisoquinolin-1(2H)-one
- UPF 1069
- 5-(2-Oxo-2-phenylethoxy)-1(2H)-isoquinolinone
- 1(2H)-Isoquinolinone, 5-(2-oxo-2-phenylethoxy)-
- UPF 1069;UPF-1069; UPF1069
- UPF 1069 10MG
- UPF1069/UPF-1069
- CS-874
- CAS:
- 1048371-03-4
- MF:
- C17H13NO3
- MW:
- 279.29
- Product Categories:
-
- Inhibitors
- Inhibitor
- Mol File:
- 1048371-03-4.mol
5-(2-Oxo-2-phenylethoxy)-3,4-dihydroisoquinolin-1(2H)-one Chemical Properties
- storage temp.
- Store at RT
- solubility
- Soluble in DMSO (up to 40 mg/ml).
- form
- solid
- color
- Off-white
- Stability:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
5-(2-Oxo-2-phenylethoxy)-3,4-dihydroisoquinolin-1(2H)-one Usage And Synthesis
Description
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
Uses
UPF 1069, is a Selective PARP-2 inhibitor.
IC 50
PARP-2: 0.3 μM (IC50); PARP-1: 8 μM (IC50)
References
[1] ROBERTO PELLICCIARI PROF. On the Way to Selective PARP-2 Inhibitors. Design, Synthesis, and Preliminary Evaluation of a Series of Isoquinolinone Derivatives[J]. ChemMedChem, 2008, 3 6: 914-923. DOI:10.1002/cmdc.200800010
[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
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