1. Cell Cycle/DNA Damage Epigenetics Stem Cell/Wnt
  2. PARP Wnt β-catenin
  3. TNKS-IN-1

TNKS-IN-1 是一种选择性强效的端锚聚合酶 (TNKS1/TNKS2) 抑制剂,其 IC50 值分别为 7.9 nM 和 8.7 nM。TNKS-IN-1 可诱导 axin2 积累,对应的 EC50 为 1500 nM。TNKS-IN-1 可通过稳定轴蛋白 (axin) 并促进 β-catenin 降解来拮抗 Wnt 信号转导通路。TNKS-IN-1 可用于结直肠癌的相关研究。

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TNKS-IN-1

TNKS-IN-1 Chemical Structure

CAS No. : 59455-93-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TNKS-IN-1 is a selective and potent tankyrase (TNKS1/TNKS2) inhibitor with IC50 values of 7.9 nM and 8.7 nM. TNKS-IN-1 induces axin2 accumulation with an EC50 of 1500 nM. TNKS-IN-1 can antagonize the Wnt signal transduction pathway by stabilizing axin proteins and promoting β-catenin degradation. TNKS-IN-1 can be used for the research of colorectal cancer[1].

IC50 & Target[1]

TNKS1

7.9 nM (IC50)

TNKS2

8.7 nM (IC50)

PARP-1

>10000 nM (IC50)

体外研究
(In Vitro)

TNKS-IN-1 (Compound 3a) (1 h) 可强效抑制纯化的人源 TNKS1 和 TNKS2,其 IC50 值分别为 7.9 nM 和 8.7 nM,且对 PARP1 的 IC50 超过 10000 nM[1]
TNKS-IN-1 (24 h) 可诱导 DLD1 细胞中 axin2 的积累,其 EC50 为 1500 nM,证实了其细胞内端锚聚合酶抑制活性[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

278.36

Formula

C18H18N2O

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-IN-1
目录号:
HY-114943
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