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Niclosamide

別名: BAY2353, Niclocide, NSC 178296 中文名稱：氯硝柳胺

Niclosamide能夠抑制DNA復(fù)制，并抑制STAT3，無細(xì)胞試驗中IC50為0.7 μM。 Niclosamide 選擇性地抑制STAT3的磷酸化，對其他同系物如STAT1和STAT5的激活沒有明顯抑制作用。

Niclosamide Chemical Structure

Niclosamide Chemical Structure

CAS: 50-65-7

規(guī)格 價格 庫存 購買數(shù)量
50mg 791.14 現(xiàn)貨
1g 1941.03 現(xiàn)貨
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Niclosamide相關(guān)產(chǎn)品

相關(guān)信號通路圖

STAT Signaling Pathways

STAT信號通路圖

細(xì)胞實驗數(shù)據(jù)示例

細(xì)胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)信息
U2OS Function assay 12.5 uM 6 hrs Induction of internalization of Frizzled1-GFP (unknown origin) expressed in human U2OS cells at 12.5 uM after 6 hrs by confocal microscopy 23453073
MDA-MB-231 Antitumor assay 75 mg/kg 5 days Antitumor activity against human ER negative MDA-MB-231 cells xenografted in nude mouse assessed as inhibition of tumor growth at 75 mg/kg, po qd for 5 days 23459613
MDA-MB-231 Antitumor assay 12.5 mg/kg 5 days Antitumor activity against human ER negative MDA-MB-231 cells xenografted in nude mouse assessed as inhibition of tumor growth at 12.5 mg/kg, ip qd for 5 days 23459613
MDA-MB-231 Antiproliferative assay 10 to 20 uM 24 hrs Antiproliferative activity against human ER negative MDA-MB-231 cells at 10 to 20 uM after 24 hrs by MTT assay 23459613
MDA-MB-231 Function assay 20 uM 24 hrs Inhibition of STAT3 promoter activity in human ER negative MDA-MB-231 cells at 20 uM after 24 hrs by dual luciferase reporter assay 23459613
MDA-MB-231 Function assay 10 uM 24 hrs Inhibition of STAT3 promoter activity in human ER negative MDA-MB-231 cells at 10 uM after 24 hrs by dual luciferase reporter assay 23459613
MDA-MB-231 Function assay 1 to 10 uM 24 hrs Inhibition of STAT3 in human ER negative MDA-MB-231 cells assessed as reduction of total STAT3 level at 1 to 10 uM after 24 hrs by Western blot analysis 23459613
MDA-MB-231 Function assay 1 to 10 uM 48 hrs Induction of morphological changes in human ER negative MDA-MB-231 cells at 1 to 10 uM after 48 hrs by light microscopic analysis 23459613
MDA-MB-231 Function assay 1 to 10 uM 48 hrs Induction of apoptosis in human ER negative MDA-MB-231 cells at 1 to 10 uM after 48 hrs by light microscopic analysis 23459613
MDA-MB-231 Antiproliferative assay 1 to 10 uM 48 hrs Antiproliferative activity against human ER negative MDA-MB-231 cells at 1 to 10 uM after 48 hrs by light microscopic analysis 23459613
MDA-MB-231 Function assay 1 to 10 uM 24 hrs Inhibition of STAT3 in human ER negative MDA-MB-231 cells assessed as reduction of phosphorylated STAT3 at Tyr-705 level at 1 to 10 uM after 24 hrs by Western blot analysis 23459613
HeLa Function assay 5 uM 24 hrs Inhibition of STAT3 in human HeLa cells at 5 uM after 24 hrs by luciferase reporter gene assay 24900231
DU145 Function assay 1 uM 2 hrs Inhibition of STAT3 nuclear translocation in EGF stimulated human DU145 cells at 1 uM administered before 100 ng/ml EGF stimulation measured after 2 hrs by confocal laser microscopy 24900231
DU145 Function assay 05 to 10 uM 2 hrs Inhibition of STAT3 interaction with DNA binding site in human DU145 cells at 05 to 10 uM after 2 hrs by EMSA 24900231
human Function assay 0.1 to 2 uM 2 hrs Decrease in cyclin D1 protein level in human DU145 cells at 0.1 to 2 uM after 2 hrs by Western blot analysis 24900231
human Function assay 0.1 to 2 uM 2 hrs Decrease in c-Myc protein level in human DU145 cells at 0.1 to 2 uM after 2 hrs by Western blot analysis 24900231
human Function assay 0.1 to 2 uM 2 hrs Decrease in Bcl-Xl protein level in human DU145 cells at 0.1 to 2 uM after 2 hrs by Western blot analysis 24900231
DU145 Function assay 0.1 to 2 uM 2 hrs Downregulation of Mcl-1 protein in human DU145 cells at 0.1 to 2 uM after 2 hrs by Western blot analysis 24900231
human Function assay 2 uM 2 hrs Inhibition of STAT3 phosphorylation at Tyr705 in human DU145 cells at 2 uM within 2 hrs by Western blot analysis 24900231
U2OS Function assay 12.5 uM 6 hrs Inhibition of Wnt/beta-catenin in human U2OS cells assessed as internalization of frizzled-GFP at 12.5 uM after 6 hrs by confocal microscopic analysis 26272032
HCT116 Function assay 5 uM 18 hrs Inhibition of Wnt/beta-catenin signaling in human HCT116 cells assessed as downregulation of cytosolic beta-catenin protein expression at 5 uM after 18 hrs by Western blot method 28233680
HCT116 Function assay 5 uM 18 hrs Inhibition of Wnt/beta-catenin signaling in human HCT116 cells assessed as downregulation of cytosolic Axin2 protein expression at 5 uM after 18 hrs by Western blot method 28233680
HCT116 Function assay 5 uM 18 hrs Inhibition of Wnt/beta-catenin signaling in human HCT116 cells assessed as downregulation of c-Myc protein expression at 5 uM after 18 hrs by Western blot method 28233680
HCT116 Function assay 5 uM 18 hrs Inhibition of Wnt/beta-catenin signaling in human HCT116 cells assessed as downregulation of Cyclin D1 protein expression at 5 uM after 18 hrs by Western blot method 28233680
HCT116 Function assay 5 uM 18 hrs Inhibition of Wnt/beta-catenin signaling in human HCT116 cells assessed as downregulation of survivin protein expression at 5 uM after 18 hrs by Western blot method 28233680
SW480 Function assay 5 uM 18 hrs Inhibition of Wnt/beta-catenin signaling in human SW480 cells assessed as downregulation of cytosolic beta-catenin protein expression at 5 uM after 18 hrs by Western blot method 28233680
SW480 Function assay 5 uM 18 hrs Inhibition of Wnt/beta-catenin signaling in human SW480 cells assessed as downregulation of cytosolic Axin2 protein expression at 5 uM after 18 hrs by Western blot method 28233680
SW480 Function assay 5 uM 18 hrs Inhibition of Wnt/beta-catenin signaling in human SW480 cells assessed as downregulation of c-Myc protein expression at 5 uM after 18 hrs by Western blot method 28233680
SW480 Function assay 5 uM 18 hrs Inhibition of Wnt/beta-catenin signaling in human SW480 cells assessed as downregulation of Cyclin D1 protein expression at 5 uM after 18 hrs by Western blot method 28233680
SW480 Function assay 5 uM 18 hrs Inhibition of Wnt/beta-catenin signaling in human SW480 cells assessed as downregulation of survivin protein expression at 5 uM after 18 hrs by Western blot method 28233680
HCT116 Function assay 2 uM 30 mins Induction of AMPK phosphorylation at Thr-172 residue in human HCT116 cells at 2 uM after 30 mins in glucose supplemented media by immunoblot method 28233680
HCT116 Function assay 2 uM 30 mins Induction of AMPK phosphorylation at Thr-172 residue in human HCT116 cells at 2 uM after 30 mins in absence of glucose by immunoblot method 28233680
HCT116 Function assay 5 uM 18 hrs Inhibition of Wnt/beta-catenin signaling pathway in human HCT116 cells cytosol lysate harboring beta-catenin mutation assessed as reduction in Axin2 protein expression at 5 uM after 18 hrs by Western blot analysis 30274939
HCT116 Function assay 5 uM 18 hrs Inhibition of Wnt/beta-catenin signaling pathway in human HCT116 cells cytosol lysate harboring beta-catenin mutation assessed as reduction in beta-catenin protein expression at 5 uM after 18 hrs by Western blot analysis 30274939
SW480 Function assay 5 uM 18 hrs Inhibition of Wnt/beta-catenin signaling pathway in human SW480 cells cytosol lysate harboring APC mutation assessed as reduction in Axin2 protein expression at 5 uM after 18 hrs by Western blot analysis 30274939
SW480 Function assay 5 uM 18 hrs Inhibition of Wnt/beta-catenin signaling pathway in human SW480 cells cytosol lysate harboring APC mutation assessed as reduction in beta-catenin protein expression at 5 uM after 18 hrs by Western blot analysis 30274939
CRC240 Function assay 5 uM 18 hrs Inhibition of Wnt/beta-catenin signaling pathway in human CRC240 cells cytosol lysate assessed as reduction in Axin2 protein expression at 5 uM after 18 hrs by Western blot analysis 30274939
CRC240 Function assay 5 uM 18 hrs Inhibition of Wnt/beta-catenin signaling pathway in human CRC240 cells cytosol lysate assessed as reduction in beta-catenin protein expression at 5 uM after 18 hrs by Western blot analysis 30274939
CCD-841-CoN Function assay 0.1 to 10 uM 2 hrs Induction of AMPK phosphorylation in human CCD-841-CoN cells at 0.1 to 10 uM after 2 hrs by Western blot analysis 30274939
RAW264.7 Cytoprotective assay 10 uM Cytoprotective activity against anthrax toxin lethal factor/protective antigen-induced cell death in mouse RAW264.7 cells assessed as cell viability at 10 uM by MTT reduction assay 19540764
CCD-841-CoN Function assay 1 uM Stimulation of mitochondrial respiration in human CCD-841-CoN cells assessed as increase in oxygen consumption rate at 1 uM in presence of FCCP by polarographic analysis 30274939
CRC240 Antitumor assay 72 mg/kg Antitumor activity against human CRC240 cells xenografted in NOD/SCID mouse at 72 mg/kg, po administered 11 days and measured on day 4, 8 during compound dosing and day 11 post last dose 30274939
HFF Antiapicomplexan assay 24 hrs Antiapicomplexan activity against Toxoplasma gondii RH tachyzoites infected in HFF cells assessed as [3H]-uracil incorporation after 24 hrs by scintillation luminescence counter, MIC50=0.2μM 22970937
HFF Antiapicomplexan assay 24 hrs Antiapicomplexan activity against Toxoplasma gondii RH tachyzoites infected in HFF cells assessed as [3H]-uracil incorporation after 24 hrs by scintillation luminescence counter, MIC90=0.2μM 22970937
Ava5 Cytotoxicity assay 3 days Cytotoxicity against human Ava5 cells after 3 days by neutral red dye assay, CC50=10μM 22059983
Ava5 Antiviral assay 3 days Antiviral activity against HCV genotype 1b infected in Ava5 cells assessed as inhibition of viral replication after 3 days by blot hybridization analysis, EC90=0.7μM 22059983
Ava5 Antiviral assay 3 days Antiviral activity against HCV genotype 1b infected in Ava5 cells assessed as inhibition of viral replication after 3 days by blot hybridization analysis, EC50=0.16μM 22059983
HEK293 Function assay 1 hr Inhibition of mitochondrial membrane potential in human HEK293 cells after 1 hr 16680159
PC3 Function assay 1 hr Inhibition of mitochondrial membrane potential in human PC3 cells after 1 hr 16680159
MIAPaCa2 Antiproliferative assay 120 hrs Antiproliferative activity against human MIAPaCa2cells after 120 hrs by MTT assay, IC50=1.1μM 16680159
LoVo Antiproliferative assay 120 hrs Antiproliferative activity against human LoVo cells after 120 hrs by MTT assay, IC50=0.7μM 16680159
U87MG Antiproliferative assay 120 hrs Antiproliferative activity against human U87MG cells after 120 hrs by MTT assay, IC50=0.4μM 16680159
A549 Antiproliferative assay 120 hrs Antiproliferative activity against human A549 cells after 120 hrs by MTT assay, IC50=0.4μM 16680159
PC3 Antiproliferative assay 120 hrs Antiproliferative activity against human PC3 cells after 120 hrs by MTT assay, IC50=0.4μM 16680159
HEK293 Function assay 8 hrs Inhibition of Wnt3A/beta-casein signaling in HEK293 cells after 8 hrs by TOPflash reporter assay, IC50=0.4μM 23453073
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against human ER negative MDA-MB-231 cells after 72 hrs by MTS assay, IC50=0.79μM 23459613
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human ER positive MCF7 cells after 72 hrs by MTS assay, IC50=1.06μM 23459613
AsPC1 Cytotoxicity assay 72 hrs Cytotoxicity against human AsPC1 cells after 72 hrs by MTS assay, IC50=1.47μM 23459613
PANC1 Cytotoxicity assay 72 hrs Cytotoxicity against human PANC1 cells after 72 hrs by MTS assay, IC50=1.73μM 23459613
MDA-MB-231 Function assay 24 hrs Inhibition of STAT3 promoter activity in human ER negative MDA-MB-231 cells after 24 hrs by dual luciferase reporter assay 23459613
HeLa Function assay 24 hrs Inhibition of STAT3 in human HeLa cells after 24 hrs by luciferase reporter gene assay, IC50=0.25μM 24900231
DU145 Antiproliferative assay 72 hrs Antiproliferative activity against human DU145 cells after 72 hrs by MTT assay, IC50=0.7μM 24900231
DU145 Growth inhibition assay 11 to 12 days Growth inhibition of human DU145 cells assessed as inhibition of colony formation after 11 to 12 days by crystal violet staining based microscopic analysis, IC50=0.7μM 24900231
HeLa Antiproliferative assay 72 hrs Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, IC50=1.4μM 24900231
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=3μM 24900231
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50=7.2μM 24900231
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells after 72 hrs by MTT assay, IC50=8.8μM 24900231
PC3 Antiproliferative assay 72 hrs Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay, IC50=11.7μM 24900231
breast cancer cells Cytotoxicity assay 72 hrs Cytotoxicity against human breast cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13μM 26272032
colon cancer cells Cytotoxicity assay 72 hrs Cytotoxicity against human colon cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13μM 26272032
lung cancer cells Cytotoxicity assay 72 hrs Cytotoxicity against human lung cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13μM 26272032
prostate cancer cells Cytotoxicity assay 72 hrs Cytotoxicity against human prostate cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13μM 26272032
ovarian cancer cells Cytotoxicity assay 72 hrs Cytotoxicity against human ovarian cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13μM 26272032
blood cancer cells Cytotoxicity assay 72 hrs Cytotoxicity against human blood cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13μM 26272032
pancreatic cancer cells Cytotoxicity assay 72 hrs Cytotoxicity against human pancreatic cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13μM 26272032
HEK293 Function assay 8 hrs Inhibition of Wnt/beta-catenin in HEK293 cells assessed as inhibition of Wnt3A-stimulated TOPFlash activity after 8 hrs, IC50=0.34μM 26272032
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTS assay, IC50=0.45μM 26272032
HCT116 Function assay 3 hrs Effect on ATP homeostasis in human HCT116 cells assessed as reduction in ATP level after 3 hrs in absence of glucose by ATP bioluminescent assay, EC50=0.056μM 28233680
HEK293 Function assay 6 hrs Inhibition of Wnt/beta-catenin signaling (unknown origin) expressed in HEK293 cells assessed as inhibition of Wnt3A-stimulated beta-catenin response transcription after 6 hrs by TOPflash dual luciferase reporter gene assay, IC50=0.12μM 28233680
HCT116 Function assay 3 hrs Effect on ATP homeostasis in human HCT116 cells assessed as reduction in ATP level after 3 hrs in absence of glucose by ATP bioluminescent assay, IC50=0.25μM 28233680
SW948 Antiproliferative assay 72 hrs Antiproliferative activity against human SW948 cells after 72 hrs by colorimetric MTS assay, IC50=0.11μM 30274939
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells after 72 hrs by colorimetric MTS assay, IC50=0.13μM 30274939
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by colorimetric MTS assay, IC50=0.41μM 30274939
HEK293 Function assay 6 hrs Inhibition of Wnt3A-stimulated Wnt/beta-catenin pathway in HEK293 cells transfected with p8xTOPFlash, Renilla luciferase plasmid pRL-TK and pLKO.1 after 6 hrs by Dual topflash luciferase reporter assay, IC50=0.45μM 30274939
CRC240 Antiproliferative assay 72 hrs Antiproliferative activity against human CRC240 cells after 72 hrs by colorimetric MTS assay, IC50=0.89μM 30274939
SW480 Antiproliferative assay 72 hrs Antiproliferative activity against human SW480 cells after 72 hrs by colorimetric MTS assay, IC50=0.98μM 30274939
DLD1 Antiproliferative assay 72 hrs Antiproliferative activity against human DLD1 cells after 72 hrs by colorimetric MTS assay, IC50=2.39μM 30274939
U2OS Function assay 6 hrs Induction of GFP-tagged Fzd1 (unknown origin) internalization expressed in human U2OS cells at 12.5 after 6 hrs by confocal microscopic method 30274939
A549 Function assay 6 hrs Induction of apoptosis in human A549 cells assessed as increase in caspase 3/7 activity after 6 hrs by caspase glo 3/7 assay 30371064
Caco2 Function assay 6 hrs Induction of apoptosis in human Caco2 cells assessed as increase in caspase 3/7 activity after 6 hrs by caspase glo 3/7 assay 30371064
AsPC1 Function assay 6 hrs Induction of apoptosis in human AsPC1 cells assessed as increase in caspase 3/7 activity after 6 hrs by caspase glo 3/7 assay 30371064
HEK293 Function assay 8 hrs Inhibition of Wnt3A-stimulated Wnt/beta-catenin pathway in HEK293 cells transfected with p8xTOPFlash, Renilla luciferase plasmid pRL-TK and pLKO.1 after 8 hrs by Dual topflash luciferase reporter gene assay, IC50=0.34μM 30551901
LN229 Antiproliferative assay 5 days Antiproliferative activity against human LN229 cells after 5 days by AlamarBlue assay, IC50=0.3μM 30583248
T98G Antiproliferative assay 5 days Antiproliferative activity against human T98G cells after 5 days by AlamarBlue assay, IC50=0.3μM 30583248
U87 Antiproliferative assay 5 days Antiproliferative activity against human U87 cells after 5 days by AlamarBlue assay, IC50=0.3μM 30583248
U138MG Antiproliferative assay 5 days Antiproliferative activity against human U138MG cells after 5 days by AlamarBlue assay, IC50=0.3μM 30583248
U373 Antiproliferative assay 5 days Antiproliferative activity against human U373 cells after 5 days by AlamarBlue assay, IC50=0.3μM 30583248
HL60 Cytotoxicity assay 3 days Cytotoxicity against human HL60 cells incubated for 3 days by CellTiter-Glo luminescent assay, IC50=0.3μM 31253529
KG1 Cytotoxicity assay 3 days Cytotoxicity against human KG1 cells incubated for 3 days by CellTiter-Glo luminescent assay, IC50=0.36μM 31253529
Jurkat Cytotoxicity assay 3 days Cytotoxicity against human Jurkat cells incubated for 3 days by CellTiter-Glo luminescent assay, IC50=0.4μM 31253529
NALM6 Cytotoxicity assay 3 days Cytotoxicity against human NALM6 cells incubated for 3 days by CellTiter-Glo luminescent assay, IC50=0.62μM 31253529
HEK293 Function assay 90 mins Inhibition of KIX-RLucN fused CBP (unknown origin) binding to KID-RLucC fused CREB (unknown origin) transfected in human HEK293 cells preincubated with compound 30 mins before before forskolin addition and measured after 90 mins in presence of coelenteraz, IC50=1.53μM 31253529
293beta5 Antiviral assay 7 days Antiviral activity against Human adenovirus 5 infected in 293beta5 cells assessed as inhibition of plaque formation incubated for 7 days by GFP reporter gene assay, IC50=0.6μM 32045239
A549 Antiviral assay 48 hrs Antiviral activity against Human adenovirus 5 infected in human A549 cells assessed as inhibition of viral entry after 48 hrs by GFP reporter gene based assay, IC50=1.22μM 32045239
A549 Cytotoxicity assay 48 hrs Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by alamar blue assay, CC50=22.9μM 32045239
Vero Antiviral assay 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr, IC50=0.28μM ChEMBL
skeletal myoblast cells Cytotoxicity assay 72 h DNDI: Cytotoxicity in Vitro, 72 hour, in rat skeletal myoblast cells, IC50=2.3μM ChEMBL
VERO-E6 Function assay 48 hrs Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of VERO-E6 cells after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging, IC50=4.1μM ChEMBL
PANC1 Cytotoxicity assay CYtotoxicity against human PANC1 cells by MTS assay, IC50=1.73μM 23416191
AsPC1 Cytotoxicity assay CYtotoxicity against human AsPC1 cells by MTS assay, IC50=1.47μM 23416191
MCF7 Cytotoxicity assay CYtotoxicity against ER-positive human MCF7 cells by MTS assay, IC50=1.06μM 23416191
MDA-MB-231 Cytotoxicity assay CYtotoxicity against ER-negative human MDA-MB-231 cells by MTS assay, IC50=0.79μM 23416191
CHO Function assay Inhibition of Bacillus anthracis anthrax protective antigen heptamer pre-pore to pore conversion in CMG2-expressing CHO cells 19540764
CHO Cytoprotective assay Cytoprotective activity against anthrax fusion toxin FP59-induced cell death in CHO cells assessed as cell viability by MTT reduction assay 19540764
Vero E6 Cytotoxicity assay Cytotoxicity against Vero E6 cells by MTT assay, CC50=22.1μM 17663539
Vero E6 Antiviral assay Antiviral activity against SARS coronavirus in Vero E6 cells assessed as inhibition of viral replication by ELISA, EC50<0.1μM 17663539
neural precursor Function assay Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay 17417631
U2OS Antiviral assay Antiviral activity against Chikungunya virus infected in human U2OS cells by RT-qPCR analysis, EC50=0.36μM 28689975
BHK-21 Antiviral assay Antiviral activity against Chikungunya virus 0611aTw infected in BHK-21 cells by RT-qPCR analysis, EC50=0.85μM 28689975
BHK-21 Antiviral assay Antiviral activity against Chikungunya virus 0810bTw infected in BHK-21 cells by RT-qPCR analysis, EC50=0.9μM 28689975
BHK-21 Antiviral assay Antiviral activity against Chikungunya virus infected in BHK-21 cells by RT-qPCR analysis, EC50=0.95μM 28689975
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
fibroblast cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells 29435139
Daoy qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for MG 63 (6-TG R) cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for RD cells 29435139
Vero Function assay Vero cells viability qHTS for Zika virus inhibitors 33229545
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生物活性

產(chǎn)品描述 Niclosamide能夠抑制DNA復(fù)制，并抑制STAT3，無細(xì)胞試驗中IC50為0.7 μM。 Niclosamide 選擇性地抑制STAT3的磷酸化，對其他同系物如STAT1和STAT5的激活沒有明顯抑制作用。
靶點
STAT3 [1]
(in Hela cells)
0.7 μM
體外研究(In Vitro)
體外研究活性 Niclosamide (< 5 μM)劑量依賴性抑制STAT3介導(dǎo)的熒光素酶報告基因活性，HeLa細(xì)胞中IC50 為0.25 μM。Niclosamide(< 2 μM)劑量依賴性抑制Du145細(xì)胞中STAT3的磷酸化。Niclosamide (1 μM)抑制Du145細(xì)胞中EGF誘導(dǎo)的STAT3的細(xì)胞核易位。Niclosamide(< 2 μM)劑量依賴性抑制Du145細(xì)胞中STAT3下游基因的轉(zhuǎn)錄。Niclosamide(< 10 μM)劑量依賴性誘導(dǎo)G0/G1期阻滯和Du145癌癥細(xì)胞的凋亡。[1]在感染SARS-CoV的Vero E6細(xì)胞中，Niclosamide在微摩爾濃度下能夠抑制SARS-CoV復(fù)制。[2] 在U2OS 細(xì)胞中，Niclosamide(< 7.5 μM)促進(jìn)Frizzled1的內(nèi)吞作用，下調(diào)Dishevelled-2蛋白，并抑制Wnt3A刺激的β-連環(huán)蛋白穩(wěn)定化和LEF/TCF報告基因活性。[3]U2OS 細(xì)胞中，Niclosamide以劑量和時間依賴的方式抑制TNF誘導(dǎo)的NF-κB報告基因活性。Niclosamide(125 nM)抑制U2OS 細(xì)胞中p65，IKKα，IKKβ，IKKγ，和TAK1誘導(dǎo)的NF-κB活化。Niclosamide(< 500 nM)完全阻斷HL-60細(xì)胞中時間和劑量依賴性TNFα誘導(dǎo)的NF-κB–DNA復(fù)合物的改變。Niclosamide(< 10 nM)抑制U266細(xì)胞中組成型NF-κB的活化。在HL-60，Molm13，或AML原代細(xì)胞中，Niclosamide以時間和劑量依賴的方式抑制TNF誘導(dǎo)的IκBα降解和p65重定位。HL-60細(xì)胞中，Niclosamide(500 nM)減少TNF誘導(dǎo)的NF-κB依賴性基因產(chǎn)物，包括細(xì)胞存活。Niclosamide劑量依賴性抑制生長，并誘導(dǎo)強烈的AML細(xì)胞凋亡，與Mcl-1和XIAP水平的減少和細(xì)胞內(nèi)ROS水平的增加相關(guān)。[4]
激酶實驗 蛋白激酶性能測定
對22中不同蛋白激酶的測定通過ProQinase Gmbh進(jìn)行。所有蛋白激酶在Sf9昆蟲細(xì)胞或大腸桿菌中以重組GST融合蛋白或組氨酸標(biāo)記的蛋白質(zhì)表達(dá)。蛋白激酶試驗GSH-瓊脂糖或Ni_NTH-瓊脂糖通過親和色譜法純化。放射性蛋白激酶試驗用于測量22種蛋白激酶的激酶活性。簡而言之，對每種蛋白激酶，50 μL反應(yīng)混合物包含60 mM HEPES-NaOH，3 mM MgCl2，3 mM MnCl2，3 μM 原礬酸鈉，1.2 mM DTT，50 μg/mL PEG20000，1 μM [γ-33P]-ATP，Niclosamide，足量酶和其底物。另外PKC-α測定包含1 mM Cacl2， 4 mM EDTA，5 μg/mL 磷脂酰絲氨酸和1 μg/mL 1, 2-二油基-丙三醇。反應(yīng)混合物在37 °C下培育60分鐘，用50 μL 2% (v/v) H3PO4停止。33Pi的整合用微板閃爍計數(shù)器測定?；钚院虸C50值使用Quattro Workflow V2.28計算。
細(xì)胞實驗 細(xì)胞系 Hela，A549，Du145，HT-29，A431，PC3細(xì)胞
濃度 16 μM
孵育時間 72小時
方法

將細(xì)胞以3-4 ×103細(xì)胞/孔的密度接種于96孔板，第二天加入包含不同濃度Niclosamide的100μL培養(yǎng)基處理。處理72小時后，將MTT加入每個孔，再培育4-5小時，吸光度在酶標(biāo)儀上570nm下測量。細(xì)胞生長抑制以樣品相對于對照組的吸光度比率評估。測定結(jié)果至少代表3個獨立實驗。
實驗圖片 檢測方法 檢測指標(biāo) 實驗圖片 PMID
Western blot β-catenin p-STAT5 / STAT5 / p-AKT / AKT / p-ERK / ERK p-BCR-ABL / BCR-ABL p-STAT3 / STAT3 / c-Myc / Survivin 27652012
Growth inhibition assay Cell viability 28418862
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 在負(fù)荷HL-60異種移植瘤的小鼠體內(nèi)，Niclosamide(40 mg/kg/d, i.p.)抑制異種移植的AML細(xì)胞生長。[4]
動物實驗 Animal Models 負(fù)荷 HL-60 異種移植瘤的裸鼠
Dosages 40 mg/kg
Administration 腹腔注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05188170 Recruiting
Acute Myeloid Leukemia (AML)
Stanford University
 November 21 2022 Phase 1
NCT04436458 Withdrawn
COVID
First Wave BioPharma Inc.
 January 20 2022 Phase 2
NCT05168644 Completed
Healthy
TFF Pharmaceuticals Inc.
 November 14 2021 Phase 1
NCT04644705 Completed
Healthy Volunteers
Charité Research Organisation GmbH|Bayer
 November 2 2020 Phase 1
NCT04592835 Unknown status
COVID-19 Patients
Daewoong Pharmaceutical Co. LTD.|Novotech (Australia) Pty Limited
 October 19 2020 Phase 1
NCT04524052 Unknown status
Healthy
Daewoong Pharmaceutical Co. LTD.
 August 2020 Phase 1

化學(xué)信息&溶解度

分子量 327.12 分子式

C13H8Cl2N2O4
CAS號 50-65-7 SDF Download Niclosamide SDF
Smiles C1=CC(=C(C=C1[N+](=O)[O-])Cl)NC(=O)C2=C(C=CC(=C2)Cl)O
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 2 mg/mL ( (6.11 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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