Niclosamide (trade name Niclocide) is a teniacide in the anthelmintic family. Niclosamide inhibits the transcription of STAT3 target genes and induces cell growth inhibition, apoptosis and cell cycle arrest of cancer cells with constitutively active STAT3. It does not decrease the level or activity of the related STAT1, STAT5, JAK or Src kinases. Niclosamide also reversibly inhibits mTORC1 signaling and stimulates autophagy in vitro. Niclosamide inhibits the transcription and DNA binding of NF-κB. It blocks tumor necrosis factor-induced IκBα phosphorylation, translocation of p65, and expression of NF-κB– regulated genes in AML cells. Niclosamide inhibits the proliferation and colony formation of Du145 prostate cancer cells, which have constitutively active STAT3, with IC50 values of 0.7 and 0.1 μM, respectively.
Int Immunopharmacol. 2024 Feb 15;128:111563.
Regulation of IL-10 expression and function by JAK-STAT in CD8+ T cells
Niclosamide purchased from AbMole
| Molecular Weight | 327.12 |
| Formula | C13H8Cl2N2O4 |
| CAS Number | 50-65-7 |
| Solubility (25°C) | DMF 4 mg/mL DMSO 3.5 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related STAT Products |
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| STAT3-IN-21, cell-permeable, negative control
STAT3-IN-21, cell-permeable, negative control, a peptide, is a negative control for Stat3 activity detection. |
| STAT3-IN-24, cell-permeable
STAT3-IN-24, cell-permeable (PpYLKTK-mts) is a STAT3 peptide inhibitor. |
| 5-FAM-GpYLPQTV-NH2
5-FAM-GpYLPQTV-NH2 is a fluorescently labeled peptide and has STAT3 inhibitory activity. |
| Ac-GpYLPQTV-NH2
Ac-GpYLPQTV-NH2 is a STAT3 inhibitor with an IC50 value of 0.33 μM. |
| XZH-5
XZH-5 inhibits the phosphorylation of STAT3 and results in the induction of apoptosis and reduction of colony forming ability. |
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