5154-02-9 Usage
Description
1,5-Isoquinolinediol, also known as an isoquinolinol, is a white to off-white solid with the chemical formula C9H7NO2. It is an isoquinoline derivative in which the hydrogens at positions 1 and 5 are replaced by hydroxy groups. 1,5-ISOQUINOLINEDIOL has been identified as a potent inhibitor of poly(ADP-ribose) polymerase (PARP; IC50 = 390 nM) and is used to study the role of PARP1 in DNA repair and oxidant stress-induced cell death.
Uses
Used in Pharmaceutical Industry:
1,5-Isoquinolinediol is used as a reagent for the preparation of PARP inhibitors. It plays a crucial role in the development of PARP inhibitors, which are essential in the treatment of various types of cancer. As a potent inhibitor of PARP (IC50 = 0.39 μM), it helps in understanding the enzyme's function in DNA repair and apoptosis, contributing to the advancement of cancer therapeutics.
Used in Research and Development:
1,5-Isoquinolinediol is used as a research tool to study the role of PARP1 in both DNA repair and oxidant stress-induced cell death. It can be employed with cells in culture and in animal models to investigate the mechanisms of PARP inhibition and its potential applications in cancer treatment.
Biochem/physiol Actions
Cell permeable: yes
Check Digit Verification of cas no
The CAS Registry Mumber 5154-02-9 includes 7 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 4 digits, 5,1,5 and 4 respectively; the second part has 2 digits, 0 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 5154-02:
(6*5)+(5*1)+(4*5)+(3*4)+(2*0)+(1*2)=69
69 % 10 = 9
So 5154-02-9 is a valid CAS Registry Number.
InChI:InChI=1/C9H7NO2/c11-8-3-1-2-7-6(8)4-5-10-9(7)12/h1-5,11H,(H,10,12)
5154-02-9Relevant articles and documents
Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds
Roth, Joshua,Madoux, Franck,Hodder, Peter,Roush, William R.
, p. 2628 - 2632 (2008/12/21)
Three synthetic routes were developed for structure-activity relationship (SAR) studies of HTS-derived isoquinolinone inhibitor probes for the orphan nuclear receptor steroidogenic factor-1 (NR5A1). Among the new analogs reported herein, 31 and 32 have im
Synthesis and Biological Activity of 4-(Diphenylmethyl)-α--1-piperazineethanol and Related Compounds
Sircar, Ila,Haleen, Steve J.,Burke, Sandra E.,Barth, Hubert
, p. 4442 - 4449 (2007/10/02)
A series of 4-(diphenylmethyl)-α--1-piperazineethanol and closely related compounds was synthesised and evaluated for cardiac and vascular activity in isolated perfused rat and guinea pig hearts.Compound 1 produced greater inotropic effects in rat hearts than in guinea pig hearts, a phenomenon which was also observed with the prototype agent DPI 201-106.Compound 15 produced an inotropic effect with one-tenth the potency of compound 1.Both compounds 1 and 15 demonstrated direct inotropic and vasodilatory effects when administered iv in anesthetized dogs, although the vasodilatory activity was more pronounced with compound 15 than 1 and DPI compound.Compound 1 lacks the CN moiety which is a key structural requirement in DPI for positive inotropic activity.The synthesis, in vitro, and in vivo evaluations of these agents, and comparative data with DPI-201-106 (compound 17) are reported.
