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XIAP-CASP7 PPI-IN-1 is a reversible inhibitor of the XIAP:CASP7 interaction, effectively disrupting the connection between XIAP and CASP7. It selectively induces apoptosis in MCF-7 and caspase-3 low-expression (CASP3/DR) triple-negative breast cancer cells. The compound overcomes chemoresistance by down-regulating β-catenin and associated ABC transporters in paclitaxel-resistant MCF-7 cells. XIAP-CASP7 PPI-IN-1 is useful for breast cancer research.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | XIAP-CASP7 PPI-IN-1 is a reversible inhibitor of the XIAP:CASP7 interaction, effectively disrupting the connection between XIAP and CASP7. It selectively induces apoptosis in MCF-7 and caspase-3 low-expression (CASP3/DR) triple-negative breast cancer cells. The compound overcomes chemoresistance by down-regulating β-catenin and associated ABC transporters in paclitaxel-resistant MCF-7 cells. XIAP-CASP7 PPI-IN-1 is useful for breast cancer research. |
| In vitro | XIAP-CASP7 PPI-IN-1 (Compound 643943) exhibits the highest cytotoxicity against MCF-7 cells at concentrations of 0-50 μM over 4-24 hours, mediated by apoptotic signaling. It binds to CASP7 via Asp93 at 0-0.5 nM μM over 24 hours, releasing active CASP7 from XIAP and inducing cell death. Additionally, at 1.25-5 μM over 24 hours, it acts synergistically with anticancer drugs, sensitizing Paclitaxel-resistant MCF-7 cells (7TR) to chemotherapy. |
| In vivo | The compound XIAP-CASP7 PPI-IN-1 (Compound 643943), administered at a dosage of 20 mg/kg intraperitoneally once daily for 2 weeks, exhibits antitumor activity in a mouse model of breast cancer. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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