Niclosamide

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

目錄號：S3030 Purity: 99.98%

Niclosamide能夠抑制DNA復制，并抑制STAT3，無細胞試驗中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

CAS: 50-65-7

規(guī)格	價格	庫存
50mg	791.14	現(xiàn)貨
1g	1941.03	現(xiàn)貨
更大包裝有超大折扣
400-668-6834 info@selleck.cn

產品質控

批次：純度： 99.98%

99.98

Niclosamide相關產品

相關靶點	STAT1 STAT3 STAT5 STAT6	點擊展開
相關產品	Stattic NSC 74859 (S3I-201) Cryptotanshinone (Tanshinone C) SH-4-54 C188-9 BP-1-102 Napabucasin (BBI608) HO-3867 Nifuroxazide AS1517499 Homoharringtonine (HHT) STAT5-IN-1 Ochromycinone (STA-21) HJC0152 APTSTAT3-9R STAT3-IN-1 SC-1 Narciclasine SH5-07 (SH-5-07) Scutellarin	點擊展開
相關化合物庫	激酶抑制劑庫 FDA藥物庫天然產物庫酪氨酸激酶抑制劑分子庫 JAK-STAT信號通路庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息
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

產品描述

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介導的熒光素酶報告基因活性，HeLa細胞中IC50 為0.25 μM。Niclosamide(< 2 μM)劑量依賴性抑制Du145細胞中STAT3的磷酸化。Niclosamide (1 μM)抑制Du145細胞中EGF誘導的STAT3的細胞核易位。Niclosamide(< 2 μM)劑量依賴性抑制Du145細胞中STAT3下游基因的轉錄。Niclosamide(< 10 μM)劑量依賴性誘導G0/G1期阻滯和Du145癌癥細胞的凋亡。^[1]在感染SARS-CoV的Vero E6細胞中，Niclosamide在微摩爾濃度下能夠抑制SARS-CoV復制。^[2] 在U2OS 細胞中，Niclosamide(< 7.5 μM)促進Frizzled1的內吞作用，下調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 細胞中，Niclosamide以劑量和時間依賴的方式抑制TNF誘導的NF-κB報告基因活性。Niclosamide(125 nM)抑制U2OS 細胞中p65，IKKα，IKKβ，IKKγ，和TAK1誘導的NF-κB活化。Niclosamide(< 500 nM)完全阻斷HL-60細胞中時間和劑量依賴性TNFα誘導的NF-κB–DNA復合物的改變。Niclosamide(< 10 nM)抑制U266細胞中組成型NF-κB的活化。在HL-60，Molm13，或AML原代細胞中，Niclosamide以時間和劑量依賴的方式抑制TNF誘導的IκBα降解和p65重定位。HL-60細胞中，Niclosamide(500 nM)減少TNF誘導的NF-κB依賴性基因產物，包括細胞存活。Niclosamide劑量依賴性抑制生長，并誘導強烈的AML細胞凋亡，與Mcl-1和XIAP水平的減少和細胞內ROS水平的增加相關。^[4]
激酶實驗	蛋白激酶性能測定
激酶實驗	對22中不同蛋白激酶的測定通過ProQinase Gmbh進行。所有蛋白激酶在Sf9昆蟲細胞或大腸桿菌中以重組GST融合蛋白或組氨酸標記的蛋白質表達。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。
細胞實驗	細胞系	Hela，A549，Du145，HT-29，A431，PC3細胞
	濃度	16 μM
	孵育時間	72小時
	方法	將細胞以3-4 ×10³細胞/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，吸光度在酶標儀上570nm下測量。細胞生長抑制以樣品相對于對照組的吸光度比率評估。測定結果至少代表3個獨立實驗。
實驗圖片	檢測方法	檢測指標	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

體內研究(In Vivo)
體內研究活性	在負荷HL-60異種移植瘤的小鼠體內，Niclosamide(40 mg/kg/d, i.p.)抑制異種移植的AML細胞生長。^[4]
動物實驗	Animal Models	負荷 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
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

參考文獻
[1] Ren X, et al. ACS Med Chem Lett, 2010, 1(9), 454-459. [2] Wu CJ, et al. Antimicrob Agents Chemother, 2004, 48(7), 2693-2696. [3] Chen M, et al. Biochemistry, 2009, 48(43), 10267-10274. [4] Jin Y, et al. Cancer Res, 2010, 70(6), 2516-2527. + 展開

參考文獻

[1] Ren X, et al. ACS Med Chem Lett, 2010, 1(9), 454-459.
[2] Wu CJ, et al. Antimicrob Agents Chemother, 2004, 48(7), 2693-2696.
[3] Chen M, et al. Biochemistry, 2009, 48(43), 10267-10274.

[4] Jin Y, et al. Cancer Res, 2010, 70(6), 2516-2527.

+ 展開

化學信息&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)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

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

DMSO : 4 mg/mL ( (12.22 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

4-Methylpyridine : 20 mg/mL (61.13 mM) Warmed with 50°C water bath;

DMSO : 4 mg/mL ( (12.22 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

DMSO : 8 mg/mL ( (24.45 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

動物體內配方計算器

實驗計算

摩爾濃度計算器

質量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內配方計算器（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）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內配方組成（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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C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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Niclosamide

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相關信號通路圖

細胞實驗數(shù)據(jù)示例

生物活性

化學信息&溶解度

實驗計算

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