1. Cell Cycle/DNA Damage Epigenetics
  2. PARP
  3. TNKS-2-IN-3

TNKS-2-IN-3 (Compound 5) 是一种选择性竞争性 Tankyrase 2 (TNKS2) 抑制剂,IC50 值为 0.3 nM,对 TNKS1 的选择性超过 20 倍,对 PARP1/2 的选择性超过 100 倍。TNKS-2-IN-3 可通过抑制 TNKS2 介导的 ADP 核糖基化来稳定轴蛋白并抑制 Wnt/β-连环蛋白通路,在结直肠癌细胞中表现出抗增殖活性。TNKS-2-IN-3 有望用于 Wnt 通路异常激活的实体瘤的研究,如结直肠癌。

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TNKS-2-IN-3

TNKS-2-IN-3 Chemical Structure

CAS No. : 2580941-64-4

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  • 生物活性

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生物活性

TNKS-2-IN-3 (Compound 5) is a selective competitive tankyrase 2 (TNKS2) inhibitor with an IC50 value of 0.3 nM, showing over 20-fold selectivity over TNKS1 and more than 100-fold selectivity over PARP1/2. TNKS-2-IN-3 stabilizes axin and suppresses the Wnt/β-catenin pathway by inhibiting TNKS2-mediated ADP-ribosylation, exhibiting antiproliferative activity in colorectal cancer cells. TNKS-2-IN-3 is proming for rasearch of solid tumors with aberrant Wnt pathway activation, such as colorectal cancer[1].

IC50 & Target

TNKS2

 

TNKS1

 

PARP1

 

PARP2

 

分子量

494.63

Formula

C24H26N6O2S2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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产品名称:
TNKS-2-IN-3
目录号:
HY-172747
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