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4H,-5H-噻吩并[2,3-c]异喹啉-5-酮

4H,-5H-噻吩并[2,3-c]异喹啉-5-酮用途

TIQ-A是一种有效的TNKS(聚ART,PARP)抑制剂,TNKS2的IC50为24 nM。TIQ-A是一种潜在的抗缺血剂[1]。

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4H,-5H-噻吩并[2,3-c]异喹啉-5-酮名称

[ CAS 号 ]:
420849-22-5

[ 中文名 ]:
4H,-5H-噻吩并[2,3-c]异喹啉-5-酮

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

[英文别名 ]:

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

4H,-5H-噻吩并[2,3-c]异喹啉-5-酮生物活性

[ 描述 ]:

TIQ-A是一种有效的TNKS(聚ART,PARP)抑制剂,TNKS2的IC50为24 nM。TIQ-A是一种潜在的抗缺血剂[1]。

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 表观遗传学 >> PARP

研究领域 >> 心血管疾病

信号通路 >> 细胞周期/DNA损伤 >> PARP

[ 靶点 ]

TNKS2:24 nM (IC50)

PARP2:210 nM (IC50)

PARP15:230 nM (IC50)

PARP10:>10 μM (IC50)

PARP14:>10 μM (IC50)

[参考文献]

[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.

4H,-5H-噻吩并[2,3-c]异喹啉-5-酮物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
282.2±9.0 °C at 760 mmHg

[ 分子式 ]:
C₁₁H₇NOS

[ 分子量 ]:
201.244

[ 闪点 ]:
124.5±18.7 °C

[ 精确质量 ]:
201.024841

[ PSA ]:
61.10000

[ LogP ]:
3.16

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.675

[ 储存条件 ]:
2-8°C

4H,-5H-噻吩并[2,3-c]异喹啉-5-酮安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H312-H332

[ 警示性声明 ]:
P280

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R20/21/22

[ 危险品运输编码 ]:
NONH for all modes of transport

4H,-5H-噻吩并[2,3-c]异喹啉-5-酮文献

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...

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