research use only
Cat.No.S8129
| Related Targets | JAK TGF-beta/Smad ERK GSK-3 ROCK Hedgehog/Smoothened PKA Secretase STAT Casein Kinase |
|---|---|
| Other Wnt/beta-catenin Inhibitors | IWR-1-endo PRI-724 (Foscenvivint) IWP-2 Tegatrabetan (BC-2059) Isoquercitrin ICG-001 SKL2001 BML-284 Hydrochloride (Wnt agonist 1, AMBMP) PNU-74654 FH535 |
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| HL60 cells | Proliferation assay | 72 h | Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.29 μM | 25644674 | ||
| MV4-11 cells | Proliferation assay | 72 h | Antiproliferative activity against human MV4-11 cells after 72 hrs, IC50=0.33 μM | 26163197 | ||
| LoVo cells | Proliferation assay | 72 h | Antiproliferative activity against human LoVo cells assessed as growth inhibition after 72 hrs by SRB method, IC50=0.36 μM | 25644674 | ||
| VCaP cells | Proliferation assay | Antiproliferative activity against human VCaP cells, EC50=0.38 μM | 23063400 | |||
| LS180 cells | Proliferation assay | 72 h | Antiproliferative activity against human LS180 cells assessed as growth inhibition after 72 hrs by SRB method, IC50=0.61 μM | 25644674 | ||
| HT-29 cells | Proliferation assay | 72 h | Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 72 hrs by SRB method, IC50=1.03 μM | 25644674 | ||
| SW707 cells | Proliferation assay | 72 h | Antiproliferative activity against human SW707 cells assessed as growth inhibition after 72 hrs by SRB method, IC50=1.73 μM | 25644674 | ||
| HL60/Vinc cells | Cytotoxicity assay | 72 h | Cytotoxicity against vincristine-resistant human HL60/Vinc cells incubated for 72 hrs by MTT assay, IC50=3.44 μM | 23079523 | ||
| BALB/3T3 cells | Cytotoxicity assay | 72 h | Cytotoxicity against mouse BALB/3T3 cells incubated for 72 hrs by MTT assay, IC50=28.08 μM | 23079523 | ||
| VCaP | Antiproliferative assay | Antiproliferative activity against human VCaP cells, EC50 = 0.38 μM. | 23063400 | |||
| HL60 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HL60 cells incubated for 72 hrs by MTT assay, IC50 = 0.44 μM. | 23079523 | ||
| LoVo | Cytotoxicity assay | 72 hrs | Cytotoxicity against human LoVo cells incubated for 72 hrs by MTT assay, IC50 = 1.11 μM. | 23079523 | ||
| HL60/Vinc | Cytotoxicity assay | 72 hrs | Cytotoxicity against vincristine-resistant human HL60/Vinc cells incubated for 72 hrs by MTT assay, IC50 = 3.44 μM. | 23079523 | ||
| LoVo/DX | Cytotoxicity assay | 72 hrs | Cytotoxicity against doxorubicin-resistant human LoVo/DX cells incubated for 72 hrs by MTT assay, IC50 = 6.23 μM. | 23079523 | ||
| BALB/3T3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BALB/3T3 cells incubated for 72 hrs by MTT assay, IC50 = 28.08 μM. | 23079523 | ||
| LoVo/DX | Antiproliferative assay | Antiproliferative activity against human LoVo/DX cells, IC50 = 1 μM. | 24631190 | |||
| HL60 | Antiproliferative assay | Antiproliferative activity against human HL60 cells, IC50 = 1.2 μM. | 24631190 | |||
| LoVo | Antiproliferative assay | Antiproliferative activity against human LoVo cells, IC50 = 1.5 μM. | 24631190 | |||
| HL60/Vinc | Antiproliferative assay | Antiproliferative activity against human HL60/Vinc cells, IC50 = 4.7 μM. | 24631190 | |||
| BALB/3T3 | Antiproliferative assay | Antiproliferative activity mouse BALB/3T3 cells, IC50 = 25.8 μM. | 24631190 | |||
| HL60 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.29 μM. | 25644674 | ||
| LoVo | Antiproliferative assay | 72 hrs | Antiproliferative activity against human LoVo cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 0.36 μM. | 25644674 | ||
| LS180 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human LS180 cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 0.61 μM. | 25644674 | ||
| LoVo/DX | Antiproliferative assay | 72 hrs | Antiproliferative activity against human doxorubicin-resistant LoVo/DX cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 0.76 μM. | 25644674 | ||
| HT-29 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 1.03 μM. | 25644674 | ||
| SW707 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SW707 cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 1.73 μM. | 25644674 | ||
| HL60/Vinc | Antiproliferative assay | 72 hrs | Antiproliferative activity against human vincristine-resistant HL60/Vinc cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 2.09 μM. | 25644674 | ||
| BALB/3T3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BALB/3T3 cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 9.33 μM. | 25644674 | ||
| MV4-11 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MV4-11 cells after 72 hrs, IC50 = 0.33 μM. | 26163197 | ||
| LoVo | Antiproliferative assay | 72 hrs | Antiproliferative activity against human LoVo cells after 72 hrs, IC50 = 0.53 μM. | 26163197 | ||
| LoVo/DX | Antiproliferative assay | 72 hrs | Antiproliferative activity against doxorubicin-resistant human LoVo/DX cells after 72 hrs, IC50 = 0.59 μM. | 26163197 | ||
| BALB/3T3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BALB/3T3 cells after 72 hrs, IC50 = 27.76 μM. | 26163197 | ||
| JIMT1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human JIMT1 cells after 72 hrs by MTT assay, IC50 = 0.52 μM. | 27326340 | ||
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 0.59 μM. | 27326340 | ||
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 2.98 μM. | 27876192 | ||
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 6.42 μM. | 27876192 | ||
| MIAPaCa2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell viability after 48 hrs by MTS assay | 28177244 | ||
| DU145 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human DU145 cells assessed as decrease in cell viability after 48 hrs by MTS assay | 28177244 | ||
| BT474 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human BT474 cells assessed as decrease in cell viability after 48 hrs by MTS assay | 28177244 | ||
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability after 48 hrs by MTS assay | 28177244 | ||
| HT-29 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HT-29 cells assessed as decrease in cell proliferation after 48 hrs by MTT assay, IC50 = 1.43 μM. | 28262526 | ||
| HGC27 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HGC27 cells assessed as decrease in cell proliferation after 48 hrs by MTT assay, IC50 = 2.57 μM. | 28262526 | ||
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell proliferation after 48 hrs by MTT assay, IC50 = 6.53 μM. | 28262526 | ||
| OV2008 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human OV2008 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 3.2 μM. | 28651817 | ||
| OV2008 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human OV2008 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50 = 4.78 μM. | 28651817 | ||
| OV2008 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human OV2008 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay, IC50 = 7.44 μM. | 28651817 | ||
| HT-29 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay, IC50 = 1.43 μM. | 28688275 | ||
| HEK293 | Cytotoxicity assay | 72 hrs | Cytotoxicity against HEK293 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.195 μM. | 29466777 | ||
| HEK293 | Cytotoxicity assay | 72 hrs | Cytotoxicity against doxycycline inducible T-Rex/K-Ras G12V HEK293 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.3295 μM. | 29466777 | ||
| HL60 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HL60 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 0.58 μM. | 29466777 | ||
| SW480 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human SW480 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 3.77 μM. | 29466777 | ||
| 4T1 | Cytotoxicity assay | 48 hrs | Cytotoxicity against mouse 4T1 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 3.78 μM. | 29466777 | ||
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 3.98 μM. | 29466777 | ||
| HeLa | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 4.49 μM. | 29466777 | ||
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 9.08 μM. | 29466777 | ||
| SMMC7721 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human SMMC7721 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 12.04 μM. | 29466777 | ||
| BEAS2B | Cytotoxicity assay | 48 hrs | Cytotoxicity against human BEAS2B cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 13.07 μM. | 29466777 | ||
| LoVo | Antiproliferative assay | 72 hrs | Antiproliferative activity against human LoVo cells after 72 hrs by SRB assay, IC50 = 0.44 μM. | 30025346 | ||
| LoVo/DX | Antiproliferative assay | 72 hrs | Antiproliferative activity against human LoVo/DX cells after 72 hrs by SRB assay, IC50 = 0.69 μM. | 30025346 | ||
| SK-BR-3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SK-BR-3 cells after 72 hrs by SRB assay, IC50 = 0.89 μM. | 30025346 | ||
| JIMT1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human JIMT1 cells after 72 hrs by SRB assay, IC50 = 1.3 μM. | 30025346 | ||
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay, IC50 = 1.5 μM. | 30025346 | ||
| ALL5 | Antiproliferative assay | 120 hrs | Antiproliferative activity against human ALL5 cells after 120 hrs by MTT assay, IC50 = 2.4 μM. | 30025346 | ||
| MCF10A | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF10A cells after 72 hrs by SRB assay, IC50 = 46 μM. | 30025346 | ||
| HMLER | Antiproliferative assay | Antiproliferative activity against HMLER cells by MTT assay Breast cancer stem cell, IC50 = 0.1 μM. | 30684870 | |||
| HeLa | Antiproliferative assay | Antiproliferative activity against human HeLa cells by MTT assay, IC50 = 0.32 μM. | 30684870 | |||
| LoVo | Antiproliferative assay | Antiproliferative activity against human LoVo cells by SRB assay, IC50 = 0.44 μM. | 30684870 | |||
| JIMT1 | Antiproliferative assay | Antiproliferative activity against human JIMT1 cells, IC50 = 0.52 μM. | 30684870 | |||
| JIMT1 | Antiproliferative assay | Antiproliferative activity against human JIMT1 cells by MTT assay, IC50 = 0.52 μM. | 30684870 | |||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells by MTT assay, IC50 = 0.59 μM. | 30684870 | |||
| LoVo/DX | Antiproliferative assay | Antiproliferative activity against human LoVo/DX cells by SRB assay, IC50 = 0.69 μM. | 30684870 | |||
| SKBR3 | Antiproliferative assay | Antiproliferative activity against human SKBR3 cells by SRB assay, IC50 = 0.89 μM. | 30684870 | |||
| HT-29 | Antiproliferative assay | Antiproliferative activity against human HT-29 cells by MTT assay, IC50 = 1.03 μM. | 30684870 | |||
| JIMT1 | Antiproliferative assay | Antiproliferative activity against human JIMT1 cells by SRB assay, IC50 = 1.3 μM. | 30684870 | |||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells by SRB assay, IC50 = 1.5 μM. | 30684870 | |||
| HGC27 | Antiproliferative assay | Antiproliferative activity against human HGC27 cells by MTT assay, IC50 = 2.57 μM. | 30684870 | |||
| HT-29 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay, IC50 = 3.21 μM. | 30684870 | ||
| 4T1 | Antiproliferative assay | Antiproliferative activity against mouse 4T1 cells by MTT assay, IC50 = 3.78 μM. | 30684870 | |||
| A549 | Antiproliferative assay | Antiproliferative activity against human A549 cells by MTT assay, IC50 = 3.98 μM. | 30684870 | |||
| MDA-MB-231 | Antiproliferative assay | Antiproliferative activity against human MDA-MB-231 cells by SRB assay, IC50 = 6.42 μM. | 30684870 | |||
| MDA-MB-231 | Antiproliferative assay | Antiproliferative activity against human MDA-MB-231 cells by MTT assay, IC50 = 6.91 μM. | 30684870 | |||
| HGC27 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HGC27 cells after 48 hrs by MTT assay, IC50 = 8.18 μM. | 30684870 | ||
| Caco2 | Antiproliferative assay | Antiproliferative activity against human Caco2 cells by MTT assay, IC50 = 12.99 μM. | 30684870 | |||
| U87 | Antiproliferative assay | Antiproliferative activity against human U87 cells by MTT assay, IC50 = 38.7 μM. | 30684870 | |||
| MCF10A | Antiproliferative assay | Antiproliferative activity against human MCF10A cells by SRB assay, IC50 = 46 μM. | 30684870 | |||
| HepG2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 24.5 μM. | 30871771 | ||
| HL60 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HL60 cells assessed as growth inhibition after 24 hrs by resazurin dye based assay, GI50 = 6.63 μM. | 30986574 | ||
| HL-60 | Function assay | 24 hrs | Trypanocidal activity against bloodstream forms of Trypanosoma brucei infected in human HL-60 cells incubated for 24 hrs followed by compound wash out after 72 hrs, GI50 = 0.18 μM. | 31103901 | ||
| MDCK | Antiviral assay | 3 days | Antiviral activity against Influenza A virus (A/Hong Kong/7/1987(H3N2)) infected in MDCK cells after 3 days by MTT assay, EC50 = 0.4 μM. | 31103901 | ||
| Vero | Antiviral assay | 24 hrs | Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr, IC50 = 0.24 μM. | ChEMBL | ||
| MIAPaCa2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MIAPaCa2 cells after 48 hrs by MTS assay, CC50 = 6.5 μM. | ChEMBL | ||
| BT474 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human BT474 cells after 48 hrs by MTS assay, CC50 = 14 μM. | ChEMBL | ||
| BT474 | Function assay | 7.5 uM | 3 days | Disruption of preformed spheroids in human BT474 cancer stem cells at 7.5 uM after 3 days by microscopic analysis | ChEMBL | |
| DU145 | Function assay | 7.5 uM | 3 days | Disruption of preformed spheroids in human DU145 cancer stem cells at 7.5 uM after 3 days by microscopic analysis | ChEMBL | |
| Click to View More Cell Line Experimental Data | ||||||
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In vitro |
DMSO
: 100 mg/mL
(133.15 mM)
Ethanol : 100 mg/mL Water : Insoluble |
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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.
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| Molecular Weight | 751.00 | Formula | C42H70O11 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 53003-10-4 | Download SDF | Storage of Stock Solutions |
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| Synonyms | Procoxacin | Smiles | CCC(C1CCC(C(O1)C(C)C(C(C)C(=O)C(CC)C2C(CC(C3(O2)C=CC(C4(O3)CCC(O4)(C)C5CCC(C(O5)C)(CC)O)O)C)C)O)C)C(=O)O | ||
| Targets/IC50/Ki |
Wnt/β-catenin
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|---|---|
| In vitro |
Salinomycin, a polyether ionophore antibiotic isolated from Streptomyces albus, has been shown to kill CSCs in different types of human cancers, most likely by interfering with ABC(ATP-binding cassette) drug transporters, the Wnt/β-catenin signaling pathway, and other CSC pathways. It exhibits antimicrobial activity against Gram-positive bacteria including Bacillus subtilis, Staphylococcus aureus, Micrococcus flavus, Sarcina lutea, Mycobacterium spp., some filamentous fungi, Plasmodium falciparum, and Eimeria spp., protozoan parasites responsible for the poultry disease coccidiosis. In addition, this compound has early been shown to act in different biological membranes, including cytoplasmic and mitochondrial membranes, as a monovalent cation ionophore with strict selectivity for alkali ions and a strong preference for K+, thereby promoting mitochondrial and cytoplasmic K+ efflux and inhibiting oxidative phosphorylation. Salinomycin can induce massive apoptosis in human cancer cells of different origin that display multiple mechanisms of drug and apoptosis resistance.
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| In vivo |
Salinomycin (from Streptomyces albus) is able to effectively eliminate CSCs and to induce partial clinical regression of heavily pretreated and therapy-resistant cancers. It has also been demonstrated as a positive ionotropic and chronotropic agent that increased cardiac output, left ventricular systolic pressure, heart rate, mean arterial pressure, coronary artery vasodilatation and blood flow, and plasma catecholamine concentration. These results have been obtained in experiments with mongrel dogs that has received a single intravenous injection of 150 μg/kg of this compound. However, It has been reported with a considerable toxicity of salinomycin in mammals, such as horses, pigs, cats, and alpacas after accidental oral or inhalative intake. Risk assessment data recently published by the European Food Safety Authority declare an acceptable daily intake (ADI) of 5 μg/kg salinomycin for humans, because daily intake of more than 500 μg/kg salinomycin by dogs leads to neurotoxic effects, such as myelin loss and axonal degeneration. Intravenous administration of 200-250 μg/kg salinomycin every second day for three weeks results in partial regression of tumor metastasis and shows only minor acute and long-term side effects, but no severe acute and long-term side effects observed with conventional chemotherapeutic drugs.
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References |
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