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  5. 1-Benzyl-I3C

1-Benzyl-I3C是一种NEDD4-1抑制剂,具有显著的抗癌活性。1-Benzyl-I3C能够直接抑制NEDD4-1的泛素化活性,其IC50为12.3μM,显著优于其前体化合物I3C的284μM。1-Benzyl-I3C及其类似物在抑制人黑色素瘤细胞增殖方面表现出良好的效果,这与它们作为NEDD4-1酶抑制剂的效力大致相关。通过结合体外泛素化实验和热稳定性分析,1-Benzyl-I3C被证明能够与NEDD4-1的催化HECT结构域结合。

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1-Benzyl-I3C Chemical Structure

1-Benzyl-I3C Chemical Structure

CAS No. : 60941-76-6

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  • 生物活性

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生物活性

1-Benzyl-I3C is a NEDD4-1 inhibitor with significant anticancer activity. 1-Benzyl-I3C can directly inhibit the ubiquitination activity of NEDD4-1 with an IC50 of 12.3μM, which is significantly better than its precursor compound I3C of 284μM. 1-Benzyl-I3C and its analogs showed good effects in inhibiting the proliferation of human melanoma cells, which is roughly related to their potency as NEDD4-1 enzyme inhibitors. By combining in vitro ubiquitination experiments and thermal stability analysis, 1-Benzyl-I3C was shown to be able to bind to the catalytic HECT domain of NEDD4-1[1].

分子量

237.30

Formula

C16H15NO

CAS 号
结构分类
初始来源
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.

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参考文献
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产品名称:
1-Benzyl-I3C
目录号:
HY-N10159
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