Niclosamide (Synonyms: NSC 178296) |
Catalog No.GC13586
One-Click Copy Product Info
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Niclosamide, an anthelmintic drug, is the small-molecule inhibitor of STAT3 with an IC50 value of 0.25±0.07μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 50-65-7
Sample solution is provided at 25 µL, 10mM.
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Niclosamide, an anthelmintic drug, is the small-molecule inhibitor of STAT3 with an IC50 value of 0.25±0.07μM[1]. Niclosamide has been widely used in cancer research and metabolic regulation studies, and is employed as a model compound to develop a series of derivatives[2].
In vitro, Niclosamide treatment for 3 days significantly inhibited the viability of HL-60 cells, with an IC50 value of 0.28 ± 0.03μM[3]. Treatment with 0.6µM Niclosamide for 24 hours significantly inhibited the expression of LRP6 in HEK293 cells and blocked the activation of the Wnt/β-catenin signaling pathway[4]. Treatment with 20μM Niclosamide for 24 hours significantly inhibited the viability of TPC-1 cells, causing the cells to become vacuolated and disintegrated[5]. Treatment with 0.5μM Niclosamide for 12 hours significantly inhibited the migration rate of BD140A cells and reduced the levels of epithelial-mesenchymal transition mediators (N-cadherin and vimentin)[6].
In vivo, Niclosamide treatment via daily intraperitoneal injection at a dose of 10mg/kg for 21 days can significantly alleviate the pulmonary fibrosis symptoms induced by bleomycin in mice and inhibit the accumulation of collagen[7]. Oral administration of Niclosamide at a dose of 200mg/kg/day for 9 weeks improved myocardial hypertrophy, cardiac fibrosis and cardiac dysfunction in mice with aortic coarctation [8].
References:
[1] Ren X, Duan L, He Q, et al. Identification of niclosamide as a new small-molecule inhibitor of the STAT3 signaling pathway[J]. ACS medicinal chemistry letters, 2010, 1(9): 454-459.
[2] Kang B, Mottamal M, Zhong Q, et al. Design, synthesis, and evaluation of niclosamide analogs as therapeutic agents for enzalutamide-resistant prostate cancer[J]. Pharmaceuticals, 2023, 16(5): 735.
[3] Chae H D, Cox N, Dahl G V, et al. Niclosamide suppresses acute myeloid leukemia cell proliferation through inhibition of CREB-dependent signaling pathways[J]. Oncotarget, 2017, 9(4): 4301.
[4] Lu W, Lin C, Roberts M J, et al. Niclosamide suppresses cancer cell growth by inducing Wnt co-receptor LRP6 degradation and inhibiting the Wnt/β-catenin pathway[J]. PloS one, 2011, 6(12): e29290.
[5] Yu K, Wang T, Li Y, et al. Niclosamide induces apoptosis through mitochondrial intrinsic pathway and inhibits migration and invasion in human thyroid cancer in vitro[J]. Biomedicine & Pharmacotherapy, 2017, 92: 403-411.
[6] Satoh K, Zhang L, Zhang Y, et al. Identification of niclosamide as a novel anticancer agent for adrenocortical carcinoma[J]. Clinical Cancer Research, 2016, 22(14): 3458-3466.
[7] Boyapally R, Pulivendala G, Bale S, et al. Niclosamide alleviates pulmonary fibrosis in vitro and in vivo by attenuation of epithelial-to-mesenchymal transition, matrix proteins & Wnt/β-catenin signaling: A drug repurposing study[J]. Life sciences, 2019, 220: 8-20.
[8] Fu Y, Hu N, Cao M, et al. Anthelmintic niclosamide attenuates pressure-overload induced heart failure in mice[J]. European Journal of Pharmacology, 2021, 912: 174614.
| Cell experiment [1]: | |
Cell lines | TPC-1 cells |
Preparation Method | The TPC-1 cells were cultured in RPIM 1640 medium containing 10% heat-inactivated fetal bovine serum (FBS) and 1% antibiotics (penicillin and streptomycin) at 37°C and 5% CO2. The exponentially growing TPC-1 cells (3000-5000 cells per well) were seeded in 96-well plates. After incubation for 24 hours, the cells were treated with different concentrations of Niclosamide (0, 1.25, 2.5, 5, 10, and 20μM). Each treatment was carried out for 24 hours, and 20μL of 5mg/mL MTT was added to each well and incubated at 37°C. The medium was removed, and 150μL DMSO was added to each well to dissolve the methylene blue. The absorbance was recorded at 570nm. |
Reaction Conditions | 0, 1.25, 2.5, 5, 10, and 20μM; 24h |
Applications | Niclosamide treatment significantly inhibited the viability of TPC-1 cells in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | Swiss albino mice |
Preparation Method | Eight-week-old male Swiss albino mice were raised in a standard environment with free access to food and water, and were maintained under a 12/12 light-dark cycle. The mice were randomly divided into the following groups (n=10): control group; Bleomycin alone group (1.5IU/kg Bleomycin); Bleomycin + Niclosamide group (10mg/kg). DMSO and polyethylene glycol 200 (in a ratio of 1:4) were used as the carrier for Niclosamide administration in the physiological saline. The DMSO concentration was 1% in the saline. The required amount of Niclosamide was weighed, dissolved in DMSO:PEG (1:4 ratio) saline, and the probes were thoroughly treated with ultrasound before administration. Mice were injected with 1.5IU/kg Bleomycin on the 0th day, and intraperitoneally injected Niclosamide once daily from the 1st to the 21st day. On the day of the end of the experiment (the 21st day), lung tissues were taken and preserved for evaluating various biochemical parameters, pathology and molecular biology studies. |
Dosage form | 10mg/kg for 21 days; i.p. |
Applications | Niclosamide treatment alleviated pulmonary fibrosis induced by bleomycin in mice. |
References: | |
| Cas No. | 50-65-7 | SDF | |
| Synonyms | NSC 178296 | ||
| Chemical Name | 5-chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzamide | ||
| Canonical SMILES | C1=CC(=C(C=C1[N+](=O)[O-])Cl)NC(=O)C2=C(C=CC(=C2)Cl)O | ||
| Formula | C13H8Cl2N2O4 | M.Wt | 327.12 |
| Solubility | ≥ 12.75mg/mL in EtOH with gentle warming; 4.55 mg/mL in DMSO (Need ultrasonic) | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.057 mL | 15.2849 mL | 30.5698 mL |
| 5 mM | 611.4 μL | 3.057 mL | 6.114 mL |
| 10 mM | 305.7 μL | 1.5285 mL | 3.057 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)