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73360-56-2

中文名稱 5-氯-N-(2-氯-4-硝基苯基)-2-羥基苯甲酰胺一水合物
英文名稱 5-Chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzamide monohydrate
CAS 73360-56-2
分子式 C13H8Cl2N2O4.H2O
分子量 345.14
MOL 文件 73360-56-2.mol
73360-56-2 結(jié)構(gòu)式 73360-56-2 結(jié)構(gòu)式

基本信息

中文別名
氯硝柳胺一水物
氯硝柳胺 一水合物
5-氯-N-(2-氯-4-硝基苯基)-2-羥基苯甲酰胺一水合物
英文別名
Zestocarp
Cestocide
2',5-D733ichloro-4'-nitrosalicylanilide Hydrate
N-(2-Chloro-4-nitrophenyl)-5-chlorosalicylaMide Hydrate
5-Chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzaMide Hydrate
5-Chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzamide monohydrate
所屬類別
分析化學(xué):農(nóng)殘、獸藥及化肥類

物理化學(xué)性質(zhì)

熔點(diǎn)224-229℃
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
形態(tài)neat

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS09
警示詞警告
危險(xiǎn)性描述H400
防范說明P273
危險(xiǎn)品標(biāo)志N
危險(xiǎn)類別碼50
安全說明61
危險(xiǎn)品運(yùn)輸編號(hào)UN 3077 9 / PGIII
WGK Germany2
RTECS號(hào)VN8400000

常見問題列表

生物活性
Niclosamide monohydrate 是一種 STAT3 抑制劑,在 HeLa 細(xì)胞中,IC50 值為 0.25 μM,可以抑制 DNA 復(fù)制。
靶點(diǎn)

STAT3

0.25 μM (IC 50 , in HeLa cells)

體外研究

Niclosamide monohydrate is an inhibitor of STAT3, inhibits STAT3-mediated luciferase reporter activity with an IC 50 of 0.25 μM in HeLa cells. Niclosamide (1 μM) inhibits the EGF-induced nuclear translocation of STAT3 in Du145 cells. Niclosamide (< 2 μM) dose dependently inhibits the transcription of STAT3 downstream genes in Du145 cells. Niclosamide (< 10 μM) induces G0/G1 arrest and apoptosis of Du145 cancer cells in a dose dependent manner. Niclosamide can block SARS-CoV replication at a micromolar concentration in Vero E6 cells infected with SARS-CoV. Niclosamide (< 7.5 μM) promotes Frizzled1 endocytosis, downregulates Dishevelled-2 protein, and inhibits Wnt3A-stimulated beta-catenin stabilization and LEF/TCF reporter activity in U2OS cells. Niclosamide inhibits the TNF-induced NF-κB reporter activity in a dose- and time-dependent manner in U2OS cells. Niclosamide (125 nM) inhibits NF-κB activation induced by p65, IKKα, IKKβ, IKKγ, and TAK1 in U2OS cells. Niclosamide (< 500 nM) completely block the time- and dose-dependent TNFα-induced alteration of the NF-κB-DNA complex in HL-60 cells. Niclosamide (< 10 nM) inhibits constitutive NF-κB activation in U266 cells. Niclosamide inhibits TNF-induced degradation of IκBα and relocation of p65 in a dose- and time-dependent manner in HL-60, Molm13, or AML primary cells. Niclosamide (500 nM) causes decrease in TNF-induced NF-κB-dependent gene products involved in cell survival in HL-60 cells. Niclosamide also inhibits the growth and induces robust apoptosis of AML cells associated with decreased Mcl-1 and XIAP levels and increased intracellular ROS levels.

體內(nèi)研究

Niclosamide (40 mg/kg/d, i.p.) suppresses growth of xenografted AML cells in nude mice bearing HL-60 xenograft tumors.

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