5-氯-N-(2-氯-4-硝基苯基)-2-羟基苯甲酰胺一水合物

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.

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