1. Metabolic Enzyme/Protease Apoptosis
  2. Phosphatase Apoptosis
  3. 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.

For research use only. We do not sell to patients.

Cu2LCl2(H2O)

Cu2LCl2(H2O) Chemical Structure

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Description

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[1].

In Vitro

[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.

Apoptosis Analysis[1]

Cell Line: HCT-116, MCF-7
Concentration: 1-25 μM
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: HCT-116
Concentration: 1-25 μM
Incubation Time: 12 h
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.
In Vivo

[Cu2LCl2(H2O)] (compound 1) (2-4 mg/kg; i.p.; repeated dosing; 21 days) exhibits dose-dependent in vivo antitumor efficacy in HCT-116 xenograft mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice (male, 6-8 weeks old, 20-25 g, subcutaneous xenograft of human HCT-116 colon cancer cells)[1]
Dosage: 2 mg/kg; 4 mg/kg
Administration: i.p.; repeated dosing; 21 days
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.
Molecular Weight

529.37

Formula

C13H15Cl2Cu2N8OS

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Cu2LCl2(H2O)
Cat. No.:
HY-183801
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