Toggle Nav
Close
  • Menu
  • Setting

Niclosamide

Catalog No.
B2283
Inhibitor of the STAT3 signaling pathway
Grouped product items
SizePriceStock Qty
5g
$48.00
In stock
10g
$76.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Niclosamide is an inhibitor of the signal transducer and activator of transcription 3 (STAT3) with IC50 value of 0.7 μM [1]. 

STATs are a class of transcription factors that regulate fundamental cellular and biological processes, such as cell proliferation, cell survival, immune responses, and angiogenesis, by modulating the expression of specific target genes. STAT3 has been frequently reported to be over-activated in various human cancer types [1]. 

In HeLa cells, Niclosamide (< 5 μM) inhibited STAT3-mediated luciferase reporter activity with in a dose dependent manner, with IC50 value of 0.25 μM. In Du145 cancer cells, Niclosamide(< 10 μM) dose-dependently induced G0/G1 arrest and apoptosis [1]. 

In nude mice bearing HL-60 xenograft tumors, Niclosamide treatment (40 mg/kg/d, i.p.) for 15 days potently inhibited the growth of HL-60 tumors. Further, immunoblotting of xenograft tissues from mice revealed a potent inhibitory effect of Niclosamide on the pathway of nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) [2]. 

References:

[1]. Ren X, Duan L, He Q, et al. Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway. ACS Medicinal Chemistry Letters, 2010, 1(9): 454-459.

[2]. Jin Y, Lu Z, Ding K, et al. Antineoplastic mechanisms of niclosamide in acute myelogenous leukemia stem cells: inactivation of the NF-kappaB pathway and generation of reactive oxygen species. Cancer Research, 2010, 70(6): 2516-2527.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt327.12
Cas No.50-65-7
FormulaC13H8Cl2N2O4
Solubilityinsoluble in H2O; ≥12.75 mg/mL in EtOH with gentle warming; ≥8.2 mg/mL in DMSO with gentle warming and ultrasonic
Chemical Name5-chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzamide
SDFDownload SDF
Canonical SMILESC1=CC(=C(C=C1[N+](=O)[O-])Cl)NC(=O)C2=C(C=CC(=C2)Cl)O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

Cell experiment:[1]

Cell lines

Du145 prostate cancer cells

Reaction Conditions

0 ~ 10 μM niclosamide for 24 h incubation

Applications

Niclosamide (≤ 2 μM) dose-dependently inhibited the Tyr-705 phosphorylation of STAT3 and the transcription of STAT3 downstream genes in Du145 cells. In addition, niclosamide induced G0/G1 arrest (≤ 1 μM) and apoptosis of Du145 cells (≤ 10 μM) in a dose dependent manner.

Animal experiment:[2]

Animal models

Nude mice bearing HL-60 xenograft tumors

Dosage form

40 mg/kg/d

Injected intraperitoneally (i.p.) for 15 days

Applications

In nude mice bearing HL-60 xenograft tumors, niclosamide treatment (40 mg/kg/d, i.p.) for 15 days potently inhibited the growth of HL-60 tumors. Further, immunoblotting of xenograft tissues from mice revealed a potent inhibitory effect of niclosamide on the NF-κB pathway.

Note

The technical data provided above is for reference only.

References:

1. Ren X, Duan L, He Q, et al. Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway. ACS Medicinal Chemistry Letters, 2010, 1(9): 454-459.

2. Jin Y, Lu Z, Ding K, et al. Antineoplastic mechanisms of niclosamide in acute myelogenous leukemia stem cells: inactivation of the NF-kappaB pathway and generation of reactive oxygen species. Cancer Research, 2010, 70(6): 2516-2527.

Quality Control