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Niclosamide-CAS 50-65-7-Calbiochem

产品编号:4061885
规格:A salicylanilide anthelmintic drug that acts as a potent and selective Stat3- and Wnt-signaling pathway inhibitor.
CAS NO:50-65-7
包装规格:1 G
产品类别:进口试剂
品牌:Sigma-Aldrich
优惠价:立即咨询
产品编号包装单位单价(元)国内现货国外库存询价单
40618851 G824
产品别名

50-65-7

Niclosamide-CAS 50-65-7-Calbiochem

5-Chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxy-benzamide, mTOR Inhibitor IX, Autophagy Inducer III, STAT3 Inhibitor XV, Wnt Pathway Inhibitor XIII

基本信息
Empirical Formula【经验(实验)分子式】
C13H8Cl2N2O4
Molecular weight
327.12
MDL number
MFCD00057597
General description【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 cells in vitro and in 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 (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.
Warning【警告】
Toxicity: Regulatory Review (Z)
Reconstitution【重悬】
Following reconstitution, aliquot and freeze (-20°C. Stock solutions are stable for up to 6 months at -20°C.
Other Notes【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.
Legal Information【法律信息】
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
产品性质
Quality Level【质量水平】
100
Assay【测定】
≥97% (HPLC)
form【形式】
solid
manufacturer/tradename
Calbiochem®
storage condition【储存条件】
OK to freeze
protect from light
color【颜色】
pale yellow
solubility【溶解性】
DMSO: 2.5 mg/mL
ethanol: 5 mg/mL
shipped in【运输】
ambient
storage temp.【储存温度】
2-8℃
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
packaging【包装】
1 g in Glass bottle
Packaged under inert gas
安全信息
Storage Class Code【储存分类代码】
11 - Combustible Solids
WGK
WGK 2
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