thieno(2,3-c)isoquinolin-5-one

Names

[ CAS No. ]:
420849-22-5

[ Name ]:
thieno(2,3-c)isoquinolin-5-one

[Synonym ]:
MFCD06407947
TIQ-A
Thieno[2,3-c]isoquinolin-5-one
PARP Inhibitor X,TIQ-A
Thieno[2,3-c]isoquinolin-5(4H)-one
thieno(2,3-c)isoquinolin-5-one

Biological Activity

[Description]:

TIQ-A is a potent TNKS (poly-ART, PARP) inhibitor, with an IC50 of 24 nM for TNKS2. TIQ-A is a potential anti-ischemic agent[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> PARP

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Cell Cycle/DNA Damage >> PARP

[Target]

TNKS2:24 nM (IC50)

PARP2:210 nM (IC50)

PARP15:230 nM (IC50)

PARP10:>10 μM (IC50)

PARP14:>10 μM (IC50)

[References]

[1]. Maksimainen MM, et al. Analogs of TIQ-A as inhibitors of human mono-ADP-ribosylating PARPs. Bioorg Med Chem. 2021 Dec 15;52:116511.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
282.2±9.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₁H₇NOS

[ Molecular Weight ]:
201.244

[ Flash Point ]:
124.5±18.7 °C

[ Exact Mass ]:
201.024841

[ PSA ]:
61.10000

[ LogP ]:
3.16

[ Vapour Pressure ]:
0.0±0.6 mmHg at 25°C

[ Index of Refraction ]:
1.675

[ Storage condition ]:
2-8°C

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H312-H332

[ Precautionary Statements ]:
P280

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xn

[ Risk Phrases ]:
R20/21/22

[ RIDADR ]:
NONH for all modes of transport

Articles

Poly(ADP-ribose) polymerase-1 inhibition prevents eosinophil recruitment by modulating Th2 cytokines in a murine model of allergic airway inflammation: a potential specific effect on IL-5.

J. Immunol. 177(9) , 6489-96, (2006)

We recently used a murine model of allergic airway inflammation to show that poly(ADP-ribose) polymerase-1 (PARP-1) plays an important role in the pathogenesis of asthma-related lung inflammation. In ...

Thieno[2,3-c]isoquinolin-5-one, a potent poly(ADP-ribose) polymerase inhibitor, promotes atherosclerotic plaque regression in high-fat diet-fed apolipoprotein E-deficient mice: effects on inflammatory markers and lipid content.

J. Pharmacol. Exp. Ther. 329(1) , 150-8, (2009)

We recently showed that poly(ADP-ribose) polymerase (PARP) is activated within atherosclerotic plaques in an animal model of atherosclerosis. Pharmacological inhibition of PARP or reduced expression i...