Copper chelator
Copper chelator is a copper chelator with anticancer activity. Copper chelator inhibits mitochondrial complex IV through copper depletion, triggering ROS/RNS stress and activating ERK/JNK/p38/AMPK, while suppressing the NRF2 antioxidant response through Keap1 upregulation. Copper chelator induces paraptosis-like death, endoplasmic reticulum stress, mitochondrial dysfunction, and ATP depletion, and inhibits cancer cell invasion and metastasis by downregulating MMP and FOSL1. Copper chelator chelates Cu (I) to form Cu complexes and releases NO with glutathione. Copper chelator inhibits the proliferation of Cu-sensitive melanoma cells and organoids as well as melanoma tumor growth in mice. Copper chelator can be used for research on melanoma.
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- CAS No.: 3101626-89-2
- Formule: C32H39N3O9S5
- Masse moléculaire:769.99
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
2.90 μM
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Cytotoxicity against human A375 melanoma cells assessed as viability reduction incubated 36 hrs by CCK-8 assay.
Cytotoxicity against human A375 melanoma cells assessed as viability reduction incubated 36 hrs by CCK-8 assay.
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42520734 |
| B16-F10 | IC50 |
10.50 μM
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Cytotoxicity against mouse B16-F10 melanoma cells assessed as viability reduction incubated 36 hrs by CCK-8 assay.
Cytotoxicity against mouse B16-F10 melanoma cells assessed as viability reduction incubated 36 hrs by CCK-8 assay.
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42520734 |
| HK-2 | IC50 |
12.33 μM
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Cytotoxicity against human HK-2 kidney cells assessed as viability reduction incubated 36 hrs by CCK-8 assay.
Cytotoxicity against human HK-2 kidney cells assessed as viability reduction incubated 36 hrs by CCK-8 assay.
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42520734 |
In Vitro
Copper chelator (4 μM; 36 h) kills A375 melanoma cells through depletion of Cu+ rather than through extracellular CCCu[1].
Copper chelator (4 μM; 36 h) induces caspase-independent non-apoptotic death in A375 melanoma cells[1].
Copper chelator (4 μM; 12-24 h) activates the MAPK pathway in A375 melanoma cells[1].
Copper chelator (4 μM; 8 h) induces paraptosis in A375 melanoma cells that requires ERK/MAPK activation[1].
Copper chelator (4 μM; 12-48 h) inhibits MMP expression and migration in A375 melanoma cells and melanoma organoids[1].
Copper chelator (4-8 μM; 48 h) reduces the growth and viability of melanoma organoids[1].
Copper chelator (4 μM; 6 h) disrupts mitochondrial integrity in A375 melanoma cells[1].
Copper chelator (4 μM; 12-24 h) induces mitochondrial dysfunction and energy stress in A375 melanoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A375 melanoma cells
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Concentration:4 μM
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Incubation Time:24 h
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Result:Downregulated C-IV expression and dramatically inhibited C-IV enzymatic activity.
Cu2+ supplementation greatly restored C-IV expression and activity.
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Cell Line:A375 melanoma cells
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Concentration:4 μM
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Incubation Time:36 h
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Result:Upregulated Keap1 and downregulated NRF2 and NQO1.
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Cell Line:A375 melanoma cells
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Concentration:4 μM
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Incubation Time:12 h and 24 h
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Result:Significantly upregulated phosphorylated ERK, JNK, and p38.
Cu2+ attenuated ERK and p38 phosphorylation, but p-JNK remained activated.
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Cell Line:A375 melanoma cells
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Concentration:4 μM
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Incubation Time:12 h and 36 h
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Result:Inhibited the migration of A375 melanoma cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, 5-6 weeks old)[1]
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Dosage:15 mg/kg; 30 mg/kg
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Administration:every two days; for 10 days
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Result:Inhibited B16-F10 tumor growth by 64.0% at 15 mg/kg and by 79.2% at 30 mg/kg.
H&E-stained tumor sections showed shrunken, decomposed, and decreased DAPI-labeled blue nuclei.
- Spheroid/Tumor Organoid Invasion Assay
- Ex Vivo Tissue Slice/Explant Invasion Assay
- Patient-Derived Organoid Invasion Assay
- Mitochondrial membrane-potential fluorescent assay
- ROS/oxidative-stress fluorescent staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- 3D Tumor Spheroid Invasion Assay
- Matrigel Transwell/Boyden Chamber Invasion Assay
- Cell Viability Determination by MTT Colorimetric Assay
- Invadopodia/Fluorescent Gelatin Degradation Assay
- Mitochondrial membrane-potential and mitochondrial mass staining
- Patient-Derived Xenograft (PDX)
- Organotypic 3D Invasion Assay
- Cell invasion
- Matrigel/ECM Transwell Invasion Assay
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- 3D Collagen/Hydrogel Matrix Invasion Assay
Chemical Information
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CAS No. 3101626-89-2
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Masse moléculaire 769.99
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Formule C32H39N3O9S5
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SMILES
CCSCCSCCN(C(C1=CC2=CC=C(C=C2OC1=O)OCCOC3=[N+](ON=C3S(=O)(C4=CC=CC=C4)=O)[O-])=O)CCSCCSCC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Copper chelator Related Classifications
HY-190512 Related Classifications
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