Cu2LCl2(H2O)
Cu2LCl2(H2O) acts as a proteasome inhibitor and protein tyrosine phosphatase inhibitor, with antiproliferative and apoptosis-inducing effects. Cu2LCl2(H2O) exhibits low cytotoxicity against normal cells and remarkable in vivo antitumor efficacy. Cu2LCl2(H2O) inhibits proteasome activity in colon cancer cells, and suppresses PTP1B and TCPTP activities in breast cancer cells. Cu2LCl2(H2O) can be used in the research of colon cancer, breast cancer and liver cancer.
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- Formule: C13H15Cl2Cu2N8OS
- Masse moléculaire:529.37
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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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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
[Cu2LCl2(H2O)] (compound 1) (0.5-25 μM; 48 h) potently inhibits proliferation of HCT-116, SW-480, HepG-2, and MCF-7 human tumor cells with IC50 values ranging from 0.68-1.94 μM after 48 h, while exhibiting high selectivity for colon cancer cells and moderate selectivity for liver cancer cells over normal human cells[1].
[Cu2LCl2(H2O)] (1-25 μM; 24 h) induces dose-dependent apoptosis in HCT-116 and MCF-7 human tumor cells after 24 h of treatment, with a more pronounced effect in HCT-116 cells[1].
[Cu2LCl2(H2O)] (1-10 μM; 12 h) induces dose-dependent accumulation of ubiquitinated proteins in HCT-116 and MCF-7 human tumor cells after 12 h of treatment at 1-10 μM, confirming functional proteasome inhibition[1].
[Cu2LCl2(H2O)] (1-25 μM; 12 h) modulates proteasome-related signaling pathways in HCT-116 human colon cancer cells after 12 h of treatment, increasing IκBα, p21, and Bax levels while decreasing NF-κB, Bcl-2, and E2F1 levels to induce apoptosis and cell cycle arrest[1].
[Cu2LCl2(H2O)] (1-25 μM; 12 h) inhibits PTP1B and TCPTP expression and activity in MCF-7 human breast cancer cells after 12 h of treatment, increasing phosphorylation of their downstream substrates to suppress tumor cell proliferation and induce apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116, MCF-7
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Concentration:1-25 μM
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Incubation Time:24 h
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Result:Increased total apoptotic cell population dose-dependently from 30.50% to 91.58% in HCT-116 cells across the concentration range.
Increased total apoptotic cell population from 11.97% to 68.88% in MCF-7 cells over the same concentration range.
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Cell Line:HCT-116
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Concentration:1-25 μM
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Incubation Time:12 h
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Result:Increased IκBα, p21, and Bax levels dose-dependently.
Decreased NF-κB, Bcl-2, and E2F1 levels dose-dependently.
Left RPN1 expression unchanged, confirming specific proteasome activity inhibition without altering core proteasome composition.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (male, 6-8 weeks old, 20-25 g, subcutaneous xenograft of human HCT-116 colon cancer cells)[1]
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Dosage:2 mg/kg; 4 mg/kg
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Administration:i.p.; repeated dosing; 21 days
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Result:Achieved a tumor inhibition rate (TIR) of 59.3% at 2 mg/kg.
Achieved a tumor inhibition rate (TIR) of 88.2% at 4 mg/kg.
Showed no significant body weight loss throughout the study period.
Chemical Information
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Masse moléculaire 529.37
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Formule C13H15Cl2Cu2N8OS
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SMILES
CC1=[N-]2N3C([N][N]([Cu]34([OH2])Cl)=C(C5=[N]4C=CN=C5)C)S[Cu+2]2(Cl)[N-]6=C1C=NC=C6
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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)
Cu2LCl2(H2O) Related Classifications
HY-183801 Related Classifications
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