1048371-03-4 Usage
Description
5-(2-Oxo-2-phenylethoxy)-3,4-dihydroisoquinolin-1(2H)-one is a chemical compound that belongs to the isoquinolinone family. It is characterized by the presence of a phenylethoxy group attached to the 5-position of the isoquinolinone core, which contributes to its unique chemical properties and potential applications.
Uses
Used in Pharmaceutical Industry:
5-(2-Oxo-2-phenylethoxy)-3,4-dihydroisoquinolin-1(2H)-one is used as a selective PARP-2 inhibitor for its potential therapeutic applications in various diseases. Its high selectivity for PARP-2 (IC50=0.3 μM) and ~27-fold selectivity against PARP-1 make it a promising candidate for targeted therapies.
Used in Neuroprotection:
In the context of neuroprotection, 5-(2-Oxo-2-phenylethoxy)-3,4-dihydroisoquinolin-1(2H)-one has been shown to increase apoptosis in hippocampal slices, which could be beneficial in certain neurological conditions. Additionally, it protects cortical cells in models of post-ischemic brain damage, suggesting its potential use in treating stroke and other ischemic injuries.
Used in Cancer Therapy:
5-(2-Oxo-2-phenylethoxy)-3,4-dihydroisoquinolin-1(2H)-one has demonstrated its ability to block the interaction between PARP-2 and FOXA1, which in turn attenuates androgen receptor-mediated gene expression. This action leads to the inhibition of androgen receptor-positive prostate cancer growth, making it a potential therapeutic agent for the treatment of prostate cancer.
References
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
Check Digit Verification of cas no
The CAS Registry Mumber 1048371-03-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,4,8,3,7 and 1 respectively; the second part has 2 digits, 0 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 1048371-03:
(9*1)+(8*0)+(7*4)+(6*8)+(5*3)+(4*7)+(3*1)+(2*0)+(1*3)=134
134 % 10 = 4
So 1048371-03-4 is a valid CAS Registry Number.