Niclosamide-CAS 50-65-7-Calbiochem

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一般描述

A cell-permeable salicylanilide that, in addition to its well-known antihelmintic efficacy, acts as a mammalian mTORC1, but not mTORC2, signaling inhibitor mechanistically distinct from rapamycin. Likely a direct consequence of autophagy activation, Niclosamide is demonstrated to induce Wnt-independent Frizzled1 and Dishevelled-2 downregulation. Unrelated to its autophagy induction activity, Niclosamide is also shown to inhibit Stat3 signaling (IC₅₀= 0.25 M in HeLa reporter assays). Efficiently inhibits breast cancer stem-like cellsin vitroandin vivo.
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 (t_1/2= 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.

包装

1 g in Glass bottle
Packaged under inert gas

警告

Toxicity: Regulatory Review (Z)

重悬

Following reconstitution, aliquot and freeze (-20°C. Stock solutions are stable for up to 6 months at -20°C.

其他说明

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.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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