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TC-H 106

TC-H 106用途

Pimelic diphenylamide 106是一种缓慢的, 结合紧密的I类HDAC抑制剂 (抑制HDAC1, 2和3, IC50值分别150 nM, 760nM, 和370 nM), 对II类HDAC没有活性。

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TC-H 106名称

[ CAS 号 ]:
937039-45-7

[ 中文名 ]:
Pimelic Diphenylamide 106

[ 英文名 ]:
TC-H 106

[英文别名 ]:

Pimelic Diphenylamide
Pimelic Diphenylamide 106
TC-H 106

TC-H 106生物活性

[ 描述 ]:

Pimelic diphenylamide 106是一种缓慢的, 结合紧密的I类HDAC抑制剂 (抑制HDAC1, 2和3, IC50值分别150 nM, 760nM, 和370 nM), 对II类HDAC没有活性。

[ 相关类别 ]:

研究领域 >> 癌症

[ 靶点 ]

HDAC1:150 nM (IC50)

HDAC3:370 nM (IC50)

HDAC2:760 nM (IC50)

HDAC8:5000 nM (IC50)

[参考文献]

[1]. Chou CJ, et al. Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I histone deacetylases. J Biol Chem. 2008 Dec 19;283(51):35402-35409.

[2]. Xu C, et al. Chemical probes identify a role for histone deacetylase 3 in Friedreich's ataxia gene silencing. Chem Biol. 2009 Sep 25;16(9):980-989.

[相关活性小分子]

TC-H 106物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
627.3±45.0 °C at 760 mmHg

[ 分子式 ]:
C₂₀H₂₅N₃O₂

[ 分子量 ]:
339.431

[ 闪点 ]:
333.1±28.7 °C

[ 精确质量 ]:
339.194672

[ PSA ]:
84.22000

[ LogP ]:
2.51

[ 外观性状 ]:
white solid

[ 蒸汽压 ]:
0.0±1.8 mmHg at 25°C

[ 折射率 ]:
1.636

[ 储存条件 ]:
-20℃

TC-H 106MSDS

详细MSDS(安全技术说明书)

TC-H 106安全信息

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

TC-H 106文献

Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).

Bioorg. Med. Chem. 23 , 5151-5, (2015)

Two of the histone deacetylases, TbDAC1 and TbDAC3, have been reported to be essential genes in trypanosomes. Therefore, we tested the activity of a panel of human histone deacetylase inhibitors (HDAC...

Inhibition of Histone Deacetylases Permits Lipopolysaccharide-Mediated Secretion of Bioactive IL-1β via a Caspase-1-Independent Mechanism.

J. Immunol. 195 , 5421-31, (2015)

Histone deacetylase (HDAC) inhibitors (HDACi) are clinically approved anticancer drugs that have important immune-modulatory properties. We report the surprising finding that HDACi promote LPS-induced...

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