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Droxinostat

Droxinostat用途

Droxinostat(NS41080)是HDAC3,HDAC6和HDAC8抑制剂,IC50分别为16.9,2.47和1.46 μM。

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Droxinostat名称

[ CAS 号 ]:
99873-43-5

[ 中文名 ]:
4-(4-氯-2-甲基苯氧基)-N-羟基丁酰胺

[ 英文名 ]:
Droxinostat

[英文别名 ]:

S1422_Selleck
cc-490
Droxinostat

Droxinostat生物活性

[ 描述 ]:

Droxinostat(NS41080)是HDAC3,HDAC6和HDAC8抑制剂,IC50分别为16.9,2.47和1.46 μM。

[ 相关类别 ]:

研究领域 >> 癌症

[ 靶点 ]

HDAC8:1.46 μM (IC50)

HDAC6:2.47 μM (IC50)

HDAC3:16.9 μM (IC50)

[参考文献]

[1]. Liu J, et al. Droxinostat, a Histone Deacetylase Inhibitor, Induces Apoptosis in Hepatocellular Carcinoma Cell Lines via Activation of the Mitochondrial Pathway and Downregulation of FLIP. Transl Oncol. 2016 Feb;9(1):70-8.

[2]. Wood TE et al. Selective inhibition of histone deacetylases sensitizes malignant cells to death receptor ligands. Mol Cancer Ther. 2010 Jan;9(1):246-56.

[3]. MMcCourt C, Maxwell P, Mazzucchelli R, Montironi R, Scarpelli M, Salto-Tellez M, O'Sullivan JM, Longley DB, Waugh DJ.,Elevation of c-FLIP in Castrate-Resistant Prostate Cancer Antagonizes Therapeutic Response to Androgen Receptor-Targeted Therapy.,Clin Cancer Res. 2012 Jul 15;18(14):3822-33. Epub 2012 May 23

[4]. Bijangi-Vishehsaraei K, Saadatzadeh MR, Huang S, Murphy MP, Safa AR.,4-(4-Chloro-2-methylphenoxy)-N-hydroxybutanamide (CMH) targets mRNA of the c-FLIP variants and induces apoptosis in MCF-7 human breast cancer cells.,Mol Cell Biochem. 2010 Sep;342(1-2):133-42. Epub 2010 May 6.

[5]. Wood TE, Dalili S, Simpson CD, Sukhai MA, Hurren R, Anyiwe K, Mao X, Suarez Saiz F, Gronda M, Eberhard Y, MacLean N, Ketela T, Reed JC, Moffat J, Minden MD, Batey RA, Schimmer AD.,Selective inhibition of histone deacetylases sensitizes malignant cells to death receptor ligands.,Mol Cancer Ther. 2010 Jan;9(1):246-56. Epub 2010 Jan 6.

[相关活性小分子]

Droxinostat物理化学性质

[ 密度 ]:
1.252 g/cm3

[ 分子式 ]:
C₁₁H₁₄ClNO₃

[ 分子量 ]:
243.68700

[ 精确质量 ]:
243.06600

[ PSA ]:
62.05000

[ LogP ]:
3.15310

[ 外观性状 ]:
white to off-white

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
DMSO: ≥20mg/mL

DroxinostatMSDS

详细MSDS(安全技术说明书)

Droxinostat安全信息

[ 符号 ]:

GHS05, GHS07

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H315-H318-H335

[ 警示性声明 ]:
P261-P280-P305 + P351 + P338

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22-37/38-41

[ 安全声明 (欧洲) ]:
26-39

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

Droxinostat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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Droxinostat相关知识

Droxinostat-作用-生物活性-靶点活性

2018-12-31 18:51:17

Droxinostat，别名NS 41080，它是HDAC的选择性抑制剂，主要用于HDAC 6和8，IC50为2.47μM和1.46μM，对HDAC3的选择性大于8倍，对HDAC1,2,4,5,7,9和10没有抑制作用。那么它的生物活性是什么？如何做实验呢？下面让小编给您详细说明。首先我们介绍Dr...