Niclosamide

Intraperitoneal injection

Hela, A549, Du145, HT-29, A431, PC3 cells

Niclosamide is currently in Phase III clinical trial in patients with colorectal cancer.

Niclosamide can inhibit DNA replication and inhibit STAT with IC50 of 0.7 uM.

DMSO

Niclosamide (< 5 uM) dose dependently inhibits STAT3-mediated luciferase reporter activity with IC50 of 0.25 in HeLa cells. Niclosamide(< 2 uM) dose dependently inhibits the phosphorylation of STAT3 in Du145 cells. Niclosamide (1 uM) inhibits the EGF-induced nuclear translocation of STAT3 in Du145 cells. Niclosamide(< 2 uM) dose dependently inhibits the transcription of STAT3 downstream genes in Du145 cells. Niclosamide(< 10 uM) dose dependently induces G0/G1 arrest and apoptosis of Du145 cancer cells. [1] Niclosamide is able to inhibit SARS-CoV replication at a micromolar concentration in Vero E6 cells infected with SARS-CoV. [2] Niclosamide(< 7.5 uM) promotes Frizzled1 endocytosis, downregulates Dishevelled-2 protein, and inhibits Wnt3A-stimulated beta-catenin stabilization and LEF/TCF reporter activity in U2OS cells. [3] Niclosamide inhibits the TNF-induced NF-kappaB reporter activity in a dose- and time-dependent manner in U2OS cells. Niclosamide(125 nM) inhibits NF-kappaB activation induced by p65, IKKalpha, IKKbeta, IKKgamma, and TAK1 in U2OS cells. Niclosamide(< 500 nM) completely block the time- and dose-dependent TNFalpha-induced alteration of the NF-kappaB–DNA complex in HL-60 cells. Niclosamide(< 10 nM) inhibits constitutive NF-kappaB activation in U266 cells. Niclosamide inhibits TNF-induced degradation of IkappaBalpha and relocation of p65 in a dose- and time-dependent manner in HL-60, Molm13, or AML primary cells. Niclosamide(500 nM) decreases TNF-induced NF-kappaB–dependent gene products involved in cell survival in HL-60 cells. Niclosamide dose dependently inhibits the growth and induces robust apoptosis of AML cells associated with decreased Mcl-1 and XIAP levels and increased intracellular ROS levels. [4]

72 hours

Cells are plated in 96-well culture plates with cell density of 3-4 x 103 cells/well and treat with Niclosamide by adding 100 uL medium containing Niclosamide of various concentrations on the second day. After 72-hour's treatment, MTT is added to each well and incubated for additional 4-5 hours, and the absorbance is measured on a microplate reader at 570nm. Cell growth inhibition is evaluated as the ratio of the absorbance of the sample to that of the control. The results are representative of at least 3 independent experiments.

Niclosamide (Niclocide) Chemical Structure

2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO