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Niclosamide
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Niclosamide图片
CAS NO:50-65-7
包装与价格：
包装价格(元)
5g电议
10g电议

产品介绍

化学性质

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
Canonical SMILESC1=CC(=C(C=C1[N+](=O)[O-])Cl)NC(=O)C2=C(C=CC(=C2)Cl)O
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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.

试验操作

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.