Snail/HDAC-IN-1

Snail/HDAC-IN-1用途

Snail/HDAC-IN-1是一种有效的Snail/HDAC双靶点抑制剂。Snail/HDAC-IN-1对HDAC1有较强的抑制活性,IC50为0.405μM,对Snail有较强的抑制作用,Kd为0.18μM。Snail/HDAC-IN-1增加HCT-116细胞中的组蛋白H4乙酰化,并降低Snail蛋白的表达,从而诱导细胞凋亡[1]。

Snail/HDAC-IN-1名称

[ CAS 号 ]:
2415281-52-4

[ 英文名 ]:
Snail/HDAC-IN-1

Snail/HDAC-IN-1生物活性

[ 描述 ]:

Snail/HDAC-IN-1是一种有效的Snail/HDAC双靶点抑制剂。Snail/HDAC-IN-1对HDAC1有较强的抑制活性,IC50为0.405μM,对Snail有较强的抑制作用,Kd为0.18μM。Snail/HDAC-IN-1增加HCT-116细胞中的组蛋白H4乙酰化,并降低Snail蛋白的表达,从而诱导细胞凋亡[1]。

[ 相关类别 ]:

研究领域 >> 癌症
信号通路 >> 细胞周期/DNA损伤 >> HDAC
信号通路 >> 表观遗传学 >> HDAC

[ 靶点 ]

HDAC1:0.405 μM (IC50)

Snail:0.18 μM (Kd)


[体外研究]

Snail/HDAC-IN-1(化合物9n)在IC50为0.0751μM的HCT-116细胞系中显示出抗增殖活性。Snail/HDAC-IN-1对NCI–H522(GI50=0.0488μM)、MDA-MB-435(GI50=0.0361μM)和MCF7(GI50=0.0518μM)显示出良好的抑制作用[1]。

[参考文献]

[1]. Cui H, et al. Design and synthesis of dual inhibitors targeting snail and histone deacetylase for the treatment of solid tumour cancer. Eur J Med Chem. 2022;229:114082.

Snail/HDAC-IN-1物理化学性质

[ 分子式 ]:
C24H21FN8OS

[ 分子量 ]:
488.54

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相关化合物

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标题:【Snail/HDAC-IN-1】Snail/HDAC-IN-1 CAS号:2415281-52-4【结构式 性质 活性】-化源网 地址:https://www.chemsrc.com/amp/cas/2415281-52-4_1705546.html