481909
Niclosamide
A salicylanilide anthelmintic drug that acts as a potent and selective Stat3- and Wnt-signaling pathway inhibitor.
别名:
Niclosamide, 5-Chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxy-benzamide, mTOR Inhibitor IX, Autophagy Inducer III, STAT3 Inhibitor XV, Wnt Pathway Inhibitor XIII
产品名称
Niclosamide, A salicylanilide anthelmintic drug that acts as a potent and selective Stat3- and Wnt-signaling pathway inhibitor.
InChI
1S/C13H8Cl2N2O4/c14-7-1-4-12(18)9(5-7)13(19)16-11-3-2-8(17(20)21)6-10(11)15/h1-6,18H,(H,16,19)
InChI key
RJMUSRYZPJIFPJ-UHFFFAOYSA-N
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
pale yellow
solubility
DMSO: 2.5 mg/mL
ethanol: 5 mg/mL
shipped in
ambient
storage temp.
2-8°C
Quality Level
Disclaimer
Toxicity: Regulatory Review (Z)
General description
A cell-permeable salicylanilide that, in addition to its well-known antihelmintic efficacy and use in tapeworm treatment, acts as a mammalian mTORC1, but not mTORC2, signaling inhibitor mechanistically distinct from rapamycin, causing MCF-7 autophagy activation under nutrient-rich conditions (by 15-fold with 4h 10 M treatment), SH-SY5Y lysosome redistribution (10 M for 8 h), and dissipation/clearance of ubiquinated protein aggregates upon proteasome inhibition in a reversible, time- and dose-dependent manner. Likely a direct consequence of autophagy activation, Niclosamide is demonstrated to induce Wnt-independent Frizzled1 endocytosis (t1/2 = 2.4 h; effective conc. <2 M) and Dishevelled-2 downregulation (IC50 ~1 M), effectively preventing Wnt3a from stimulating HEK293 cellular LEF/TCF transcription activity (IC50 = 0.5 M TOPFlash reporter assays). Unrelated to its autophagy induction activity, Niclosamide is also shown to inhibit Stat3 signaling (IC50 = 0.25 M in HeLa-based pLucTKS3 reporter assays) by suppressing the phosphorylation of Jak1 Tyr1022/1023 (2 h treatment at 0.5 to 2.0 M in Du145 cultures) and Stat3 Tyr705 (by >90% after 24 h treatment at 2 and 5 M, respectively, in Du145 and HeLa cultures), without affecting the phosphorylation of Stat1 Tyr701, Stat3 Ser727, Stat5 Tyr694, or Jak2 Tyr1007/1008.
Other Notes
Wang, Y.C., et al. 2013. PLoS ONE8, e74538.
Chen, W., et al. 2010. Am. J. Physiol. Gastrointest. Liver Physiol.299, G293.
Gies, E., et al. 2010. PLoS ONE5, e14410.
Ren, X., et al. 2010. ACS Med. Chem. Lett.1, 454.
Chen, M., et al. 2009. Biochemistry48, 10267.
Chen, W., et al. 2010. Am. J. Physiol. Gastrointest. Liver Physiol.299, G293.
Gies, E., et al. 2010. PLoS ONE5, e14410.
Ren, X., et al. 2010. ACS Med. Chem. Lett.1, 454.
Chen, M., et al. 2009. Biochemistry48, 10267.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C. Stock solutions are stable for up to 6 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Jiuge Tang et al.
International journal of molecular sciences, 25(8) (2024-04-27)
Canonical autophagy is an evolutionarily conserved process that forms double-membrane structures and mediates the degradation of long-lived proteins (LLPs). Noncanonical autophagy (NCA) is an important alternative pathway involving the formation of microtubule-associated protein 1 light chain 3 (LC3)-positive structures that
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