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Cat.No.S4290
| Related Targets | CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor TRP Channel GluR |
|---|---|
| Other ATPase Products | (-)-Blebbistatin Thapsigargin Brefeldin A (BFA) CB-5083 Sodium orthovanadate Golgicide A BTB06584 Ginsenoside Rb1 CDN1163 Periplocin |
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| rat hepatocytes | Function assay | Drug uptake in rat hepatocytes, Km=0.18 μM | 20926619 | |||
| human hepatocytes | Function assay | 0.05 to 10 uM | Drug uptake in sandwich-cultured human hepatocytes at 0.05 to 10 uM at 37 degC by Michaelis-Menten kinetics/scintillation spectroscopy, Km=2.39 μM | 20926619 | ||
| LLC-PK1 | Function assay | TP_TRANSPORTER: inhibition of E217betaG uptake in Oatp2-expressing LLC-PK1 cells, Ki=0.037μM | 11408557 | |||
| High Five (BTI-TN5B1-4) | Function assay | TP_TRANSPORTER: ATP hydrolysis in membrane fraction from High Five (BTI-TN5B1-4) cells, Km=25.9μM | 11785684 | |||
| LLC-PK1 | Function assay | TP_TRANSPORTER: inhibition of Taurocholate uptake in Oatp2-expressing LLC-PK1 cells, Ki=0.58μM | 11792694 | |||
| LLC-PK1 | Function assay | TP_TRANSPORTER: uptake in Oatp2-expressing LLC-PK1 cells, Km=1.07μM | 11792694 | |||
| LLC-PK1 | Function assay | TP_TRANSPORTER: uptake in Oatp2-expressing LLC-PK1 cells, Km=0.279μM | 11883641 | |||
| MDCK | Function assay | TP_TRANSPORTER: cell accumulation in OATP4C1-expressing MDCK cells, Km=7.8μM | 14993604 | |||
| MDCK | Function assay | TP_TRANSPORTER: cell accumulation in OATP4C1-expressing MDCK cells, Km=8μM | 14993604 | |||
| TK10 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human TK10 cells after 48 hrs by SRB assay, IC50=0.0146μM | 16309315 | ||
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay, IC50=0.0241μM | 16309315 | ||
| K562 | Cytotoxicity assay | Cytotoxicity against human K562 cells by XTT assay, IC50=0.0282μM | 16309315 | |||
| UACC62 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human UACC62 cells after 48 hrs by SRB assay, IC50=0.0295μM | 16309315 | ||
| HeLa | Cytotoxicity assay | Cytotoxicity against human HeLa cells assessed as inhibition of DNA replication by imaging analysis | 18066055 | |||
| HeLa | Function assay | Inhibition of mitosis in human HeLa cells by imaging analysis | 18066055 | |||
| colon cancer | Cytotoxicity assay | 72 hrs | Cytotoxicity against human colon cancer cells after 72 hrs by FMCA method, IC50=0.1μM | 19894733 | ||
| CC20 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human CC20 cells after 72 hrs by FMCA method, IC50=0.24μM | 19894733 | ||
| HCT116 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCT116 cells after 72 hrs by FMCA method, IC50=0.27μM | 19894733 | ||
| HT-29 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HT-29 cells after 72 hrs by FMCA method, IC50=1.4μM | 19894733 | ||
| Hs578Bst | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Hs578Bst cells after 72 hrs by CellTiter-Glo assay, IC50=0.04μM | 22316168 | ||
| Hs578T | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Hs578T cells after 72 hrs by CellTiter-Glo assay, IC50=0.251μM | 22316168 | ||
| T47D | Cytotoxicity assay | 72 hrs | Cytotoxicity against human T47D cells after 72 hrs by CellTiter-Glo assay, IC50=0.66μM | 22316168 | ||
| SK-BR-3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SK-BR-3 cells after 72 hrs by CellTiter-Glo assay, IC50=1.08μM | 22316168 | ||
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells after 72 hrs by CellTiter-Glo assay, IC50=4.7μM | 22316168 | ||
| Hs578Bst | Cytotoxicity assay | 40 uM | 72 hrs | Cytotoxicity against human Hs578Bst cells at 40 uM after 72 hrs by CellTiter-Glo assay relative to untreated control, IC50=47.7μM | 22316168 | |
| CHO | Function assay | pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells, IC50=3.23594μM | 23571415 | |||
| CHO | Function assay | pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells, IC50=13.1826μM | 23571415 | |||
| Hs683 | Cytotoxicity assay | 3 days | Cytotoxicity against human Hs683 cells after 3 days by MTT assay, IC50=0.04μM | 23706005 | ||
| A549 | Cytotoxicity assay | 3 days | Cytotoxicity against human A549 cells after 3 days by MTT assay, IC50=0.05μM | 23706005 | ||
| PC3 | Cytotoxicity assay | 3 days | Cytotoxicity against human PC3 cells after 3 days by MTT assay, IC50=0.075μM | 23706005 | ||
| U373 | Cytotoxicity assay | 3 days | Cytotoxicity against human U373 cells after 3 days by MTT assay, IC50=0.146μM | 23706005 | ||
| SK-MEL-28 | Cytotoxicity assay | 3 days | Cytotoxicity against human SK-MEL-28 cells after 3 days by MTT assay, IC50=0.266μM | 23706005 | ||
| MCF7 | Cytotoxicity assay | 3 days | Cytotoxicity against human MCF7 cells after 3 days by MTT assay, IC50=0.426μM | 23706005 | ||
| Drosophila Schneider cells | Function assay | Antagonist activity at transactivation domain of RORgammat (unknown origin) expressed in Drosophila Schneider cells co-expressing Gal4-DNA binding domain, IC50=2μM | 24040486 | |||
| Drosophila Schneider cells | Function assay | Antagonist activity at transactivation domain of RORgammat (unknown origin) expressed in Drosophila Schneider cells co-expressing Gal4-DNA binding domain, IC50=2μM | 24040486 | |||
| RKO-AS45-1 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human RKO-AS45-1 cells after 48 hrs by MTT assay, IC50=0.42μM | 26122772 | ||
| HeLa | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50=2.2μM | 26122772 | ||
| HeLa | Function assay | 150 nM | 24 hrs | Inhibition of Na(+)/K(+) ATPase in human HeLa cells at 150 nM after 24 hrs by immunoblotting | 26122772 | |
| HeLa | Function assay | 150 nM | 24 hrs | Inhibition of Na(+)/K(+) ATPase in human HeLa cells at 150 nM after 24 hrs by immunoblotting | 26122772 | |
| HeLa | Function assay | 150 nM | 24 hrs | Inhibition of Na(+)/K(+) ATPase in human HeLa cells at 150 nM after 24 hrs by immunoblotting | 26122772 | |
| HeLa | Function assay | 150 nM | 24 hrs | Inhibition of Na(+)/K(+) ATPase in human HeLa cells at 150 nM after 24 hrs by immunoblotting | 26122772 | |
| HeLa | Function assay | 150 nM | 24 hrs | Inhibition of Na(+)/K(+) ATPase in human HeLa cells at 150 nM after 24 hrs by immunoblotting | 26122772 | |
| HeLa | Function assay | 150 nM | 24 hrs | Inhibition of Na(+)/K(+) ATPase in human HeLa cells at 150 nM after 24 hrs by immunoblotting | 26122772 | |
| HeLa | Function assay | 150 nM | 24 hrs | Inhibition of Na(+)/K(+) ATPase in human HeLa cells at 150 nM after 24 hrs by immunoblotting | 26122772 | |
| HeLa | Function assay | 150 nM | 24 hrs | Inhibition of Na(+)/K(+) ATPase in human HeLa cells at 150 nM after 24 hrs by immunoblotting | 26122772 | |
| Kasumi-1 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human Kasumi-1 cells incubated for 48 hrs by MTS assay, IC50=0.093μM | 27983842 | ||
| MV4-11 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MV4-11 cells incubated for 48 hrs by MTS assay, IC50=0.111μM | 27983842 | ||
| HT-29 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HT-29 cells incubated for 72 hrs by SRB assay, IC50=0.38μM | 27983842 | ||
| H1299 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human H1299 cells incubated for 24 hrs by MTT assay, IC50=0.46μM | 27983842 | ||
| CCD-112CoN | Cytotoxicity assay | 72 hrs | Cytotoxicity against human CCD-112CoN cells incubated for 72 hrs, IC50=2.4μM | 27983842 | ||
| DU145 | Function assay | 50 uM | 5 hrs | Inhibition of Na+/K+ ATPase pump in human DU145 cells assessed as increase in intracellular calcium level at 50 uM measured after 5 hrs by Fura-2/AM dye based fluorescence assay | 31120251 | |
| DU145 | Function assay | 50 uM | 5 hrs | Inhibition of Na+/K+ ATPase pump in human DU145 cells assessed as increase in intracellular calcium level at 50 uM measured after 5 hrs by Fura-2/AM dye based fluorescence assay | 31120251 | |
| DU145 | Function assay | 50 uM | 5 hrs | Inhibition of Na+/K+ ATPase pump in human DU145 cells assessed as increase in intracellular calcium level at 50 uM measured after 5 hrs by Fura-2/AM dye based fluorescence assay | 31120251 | |
| DU145 | Function assay | 50 uM | 5 hrs | Inhibition of Na+/K+ ATPase pump in human DU145 cells assessed as increase in intracellular calcium level at 50 uM measured after 5 hrs by Fura-2/AM dye based fluorescence assay | 31120251 | |
| DU145 | Function assay | 50 uM | 5 hrs | Inhibition of Na+/K+ ATPase pump in human DU145 cells assessed as increase in intracellular calcium level at 50 uM measured after 5 hrs by Fura-2/AM dye based fluorescence assay | 31120251 | |
| DU145 | Function assay | 50 uM | 5 hrs | Inhibition of Na+/K+ ATPase pump in human DU145 cells assessed as increase in intracellular calcium level at 50 uM measured after 5 hrs by Fura-2/AM dye based fluorescence assay | 31120251 | |
| DU145 | Function assay | 50 uM | 5 hrs | Inhibition of Na+/K+ ATPase pump in human DU145 cells assessed as increase in intracellular calcium level at 50 uM measured after 5 hrs by Fura-2/AM dye based fluorescence assay | 31120251 | |
| DU145 | Function assay | 50 uM | 5 hrs | Inhibition of Na+/K+ ATPase pump in human DU145 cells assessed as increase in intracellular calcium level at 50 uM measured after 5 hrs by Fura-2/AM dye based fluorescence assay | 31120251 | |
| Click to View More Cell Line Experimental Data | ||||||
|
In vitro |
DMSO
: 100 mg/mL
(128.05 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.
| Molecular Weight | 780.94 | Formula | C41H64O14 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 20830-75-5 | Download SDF | Storage of Stock Solutions |
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| Synonyms | NSC 95100, 12β-Hydroxydigitoxin | Smiles | CC1C(C(CC(O1)OC2C(OC(CC2O)OC3C(OC(CC3O)OC4CCC5(C(C4)CCC6C5CC(C7(C6(CCC7C8=CC(=O)OC8)O)C)O)C)C)C)O)O | ||
| Targets/IC50/Ki |
Na,K-ATPase α2β3
42.8 nM(Ki)
Na,K-ATPase α2β1
58.7 nM(Ki)
Na,K-ATPase α1β1
268 nM(Ki)
|
References |
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| Methods | Biomarkers | Images | PMID |
|---|---|---|---|
| Western blot | p-Src / Src / p-EGFR / EGFR / p-STAT3 / STAT3 p-PI3K / PI3K / p-AKT / AKT / p-MEK / MEK / p-ERK / ERK / p-FAK / FAK / p-SAPK/JNK / p-Paxillin / Paxillin / p-p130Cas / p130Cas Nrf2 |
|
25955608 |
| Growth inhibition assay | Cell viability |
|
25955608 |
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