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Niclosamide STAT remmer

Name: Niclosamide
Brand: Selleck Chemicals
SKU: S3030
Rating: 5 (54 reviews)

Cat.nr.S3030

Niclosamide kan de DNA-replicatie remmen en STAT3 remmen met een IC50 van 0,7 μM in een celvrije test. Deze verbinding remde selectief de fosforylering van STAT3 en had geen duidelijke remming tegen de activering van andere homologen (bijv. STAT1 en STAT5).

Niclosamide STAT remmer Chemical Structure

Chemische structuur

Molecuulgewicht: 327.12

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Kwaliteitscontrole

Batch: Zuiverheid: 99.98%

99.98

Gerelateerde doelwitten	EGFR JAK Pim
Overig STAT Inhibitoren	Napabucasin (BBI608) Stattic NSC 74859 (S3I-201) Cryptotanshinone (Tanshinone C) C188-9 (TTI-101) SH-4-54 BP-1-102 AS1517499 Nifuroxazide HO-3867

Celkweek, behandeling & werkzame concentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
PC3	Antiproliferative assay		120 hrs	Antiproliferative activity against human PC3 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
U87MG	Antiproliferative assay		120 hrs	Antiproliferative activity against human U87MG cells after 120 hrs by MTT assay, IC50=0.4μM	16680159
LoVo	Antiproliferative assay		120 hrs	Antiproliferative activity against human LoVo cells after 120 hrs by MTT assay, IC50=0.7μM	16680159
MIAPaCa2	Antiproliferative assay		120 hrs	Antiproliferative activity against human MIAPaCa2cells after 120 hrs by MTT assay, IC50=1.1μM	16680159
PC3	Function assay		1 hr	Inhibition of mitochondrial membrane potential in human PC3 cells after 1 hr	16680159
HEK293	Function assay		1 hr	Inhibition of mitochondrial membrane potential in human HEK293 cells after 1 hr	16680159
neural precursor	Function assay			Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay	17417631
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
Vero E6	Cytotoxicity assay			Cytotoxicity against Vero E6 cells by MTT assay, CC50=22.1μM	17663539
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
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
CHO	Function assay			Inhibition of Bacillus anthracis anthrax protective antigen heptamer pre-pore to pore conversion in CMG2-expressing CHO cells	19540764
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
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	Cytotoxicity assay		3 days	Cytotoxicity against human Ava5 cells after 3 days by neutral red dye assay, CC50=10μM	22059983
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
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
MDA-MB-231	Cytotoxicity assay			CYtotoxicity against ER-negative human MDA-MB-231 cells by MTS assay, IC50=0.79μM	23416191
MCF7	Cytotoxicity assay			CYtotoxicity against ER-positive human MCF7 cells by MTS assay, IC50=1.06μM	23416191
AsPC1	Cytotoxicity assay			CYtotoxicity against human AsPC1 cells by MTS assay, IC50=1.47μM	23416191
PANC1	Cytotoxicity assay			CYtotoxicity against human PANC1 cells by MTS assay, IC50=1.73μM	23416191
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
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	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	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		24 hrs	Inhibition of STAT3 promoter activity in human ER negative MDA-MB-231 cells after 24 hrs by dual luciferase reporter 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		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
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
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
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		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
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
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
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
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	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
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
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
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	Function assay			Vero cells viability qHTS for Zika virus inhibitors	33229545
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
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit

Molecuulgewicht	327.12	Formule	C₁₃H₈Cl₂N₂O₄	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	50-65-7	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	BAY2353, Niclocide, NSC 178296			Smiles	C1=CC(=C(C=C1[N+](=O)[O-])Cl)NC(=O)C2=C(C=CC(=C2)Cl)O

Oplosbaarheid

In vitro
Batch:

DMSO : 2 mg/mL (6.11 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	10% DMSO 1 40% PEG 300 2 5%Tween80 3 45%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	0.200mg/ml (0.61mM)	Taking the 1 mL working solution as an example, add 100 μL of 2 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC₅₀/Ki	STAT3 (in Hela cells) 0.7 μM
In vitro	Niclosamide (< 5 μM) remt dosisafhankelijk de STAT3-gemedieerde luciferase reporteractiviteit met een IC50 van 0,25 μM in HeLa-cellen. Deze verbinding (< 2 μM) remt dosisafhankelijk de fosforylering van STAT3 in Du145-cellen. Het (1 μM) remt de EGF-geïnduceerde nucleaire translocatie van STAT3 in Du145-cellen. Deze chemische stof (< 2 μM) remt dosisafhankelijk de transcriptie van stroomafwaartse STAT3-genen in Du145-cellen. Het (< 10 μM) induceert dosisafhankelijk G0/G1-arrest en apoptose van Du145-kankercellen. Deze verbinding is in staat de SARS-CoV-replicatie te remmen bij een micromolaire concentratie in Vero E6-cellen geïnfecteerd met SARS-CoV. Het (< 7,5 μM) bevordert Frizzled1-endocytose, reguleert Dishevelled-2-eiwit omlaag en remt Wnt3A-gestimuleerde bèta-catenine-stabilisatie en LEF/TCF-reporteractiviteit in U2OS-cellen. Deze chemische stof remt de TNF-geïnduceerde NF-κB-reporteractiviteit op een dosis- en tijdsafhankelijke manier in U2OS-cellen. Het (125 nM) remt NF-κB-activering geïnduceerd door p65, IKKα, IKKβ, IKKγ en TAK1 in U2OS-cellen. Deze verbinding (< 500 nM) blokkeert volledig de tijd- en dosisafhankelijke TNFα-geïnduceerde verandering van het NF-κB–DNA-complex in HL-60-cellen. Het (< 10 nM) remt constitutieve NF-κB-activering in U266-cellen. Deze chemische stof remt TNF-geïnduceerde afbraak van IκBα en verplaatsing van p65 op een dosis- en tijdsafhankelijke manier in HL-60-, Molm13- of primaire AML-cellen. Het (500 nM) vermindert TNF-geïnduceerde NF-κB-afhankelijke genproducten die betrokken zijn bij celoverleving in HL-60-cellen. Deze verbinding remt dosisafhankelijk de groei en induceert robuuste apoptose van AML-cellen geassocieerd met verlaagde Mcl-1- en XIAP-niveaus en verhoogde intracellulaire ROS-niveaus.
Kinase Assay	Eiwitkinase-profileringstest
Kinase Assay	De test voor 22 verschillende eiwitkinasen wordt uitgevoerd door ProQinase Gmbh. Alle eiwitkinasen worden ofwel in Sf9-insectencellen ofwel in E.coli tot expressie gebracht als recombinante GST-fusie-eiwitten of His-getagde eiwitten. Eiwitkinasen worden gezuiverd door affiniteitschromatografie met behulp van ofwel GSH-agarose of Ni_NTH-agarose. Een radiometrische eiwitkinasetest wordt gebruikt voor het meten van de kinaseactiviteit van de 22 eiwitkinasen. Kortom, voor elke eiwitkinase een 50 μL reactiecocktail die 60 mM HEPES-NaOH, 3 mM MgCl₂, 3 mM MnCl₂, 3 μM Na-orthovanadaat, 1,2 mM DTT, 50 μg/mL PEG20000, 1 μM [γ-33P]-ATP, Niclosamide, voldoende hoeveelheid enzym en zijn substraat bevat. De PKC-alpha test bevat bovendien 1 mM CaCl₂, 4 mM EDTA, 5 μg/mL fosfatidylserine en 1 μg/mL 1,2-Dioleyl-glycerol. De reactiecocktails worden gedurende 60 minuten bij 37 °C geïncubeerd en gestopt met 50 μL 2% (v/v) H₃PO₄. De incorporatie van 33Pi wordt bepaald met een microplaatscintillatieteller. De activiteiten en de IC50-waarden worden berekend met behulp van Quattro Workflow V2.28.
In vivo	Niclosamide (40 mg/kg/dag, i.p.) remt de groei van xenogetransplanteerde AML-cellen in naakte muizen met HL-60-xenografttumoren.
Referenties	[1] http://pubs.acs.org/doi/full/10.1021/ml100146z [2] https://pubmed.ncbi.nlm.nih.gov/15215127/ [3] https://pubmed.ncbi.nlm.nih.gov/19772353/ [4] https://pubmed.ncbi.nlm.nih.gov/20215516/

Toepassingen

Methoden	Biomarkers	Afbeeldingen	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

Informatie over klinische proeven

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
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

Technische ondersteuning

Gebruiksaanwijzing

Tel: +1-832-582-8158 Ext:3

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