481909
Niclosamide
A salicylanilide anthelmintic drug that acts as a potent and selective Stat3- and Wnt-signaling pathway inhibitor.
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所有图片(1)
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
经验公式（希尔记法）:
C13H8Cl2N2O4
推荐产品
质量水平
检测方案
≥97% (HPLC)
形式
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
pale yellow
溶解性
DMSO: 2.5 mg/mL
ethanol: 5 mg/mL
运输
ambient
储存温度
2-8°C
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
一般描述
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.
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.
包装
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.
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
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°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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