XIAP-CASP7 PPI-IN-1
Xiap-casp7 PPI-IN-1 is a reversible XIAP: CASP7 inhibitor with specifically disrupting the interaction between XIAP and CASP7. XIAP-CASP7 PPI-IN-1 selectively induce MCF-7 and other caspase-3 down-regulation (CASP3/DR) triple-negative breast cancer cell apoptosis. XIAP-CASP7 PPI-IN-1 overcomes chemoresistance via down-regulating β-catenin and its associated ABC transporters in Paclitaxel (HY-B0015)-resistant MCF-7 cells. XIAP-CASP7 PPI-IN-1 can be used for the study of breast cancer.
For research use only. We do not sell to patients.
- Formula: C25H21N3O3
- Molecular Weight:411.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
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All Caspase Isoforms
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Biological Activity
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Caspase-3 |
Caspase-7 |
Caspase-9 |
XIAP-CASP7 PPI-IN-1 (Compound 643943) (0-50 μM, 4-24 h) exhibits the greatest cytotoxicity against MCF-7, and this toxic effect is mediated by apoptotic signaling.[1].
XIAP-CASP7 PPI-IN-1 (0-0.5 μM, 24 h) binds with CASP7 through Asp93 and activates CASP7 from XIAP:CASP7, thereby inducing cell death[1].
XIAP-CASP7 PPI-IN-1 (1.25-5 μM, 24 h) exhibits synergistic effect with anti-cancer drugs and effectively sensitizes Paclitaxel-resistant MCF-7 cells (7TR) cancer cells to chemotherapy[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Paclitaxel-resistant MCF-7 cells (7TR)
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Concentration:1.25, 2.5 and 5 μM alone or with Staurosporine (STS) (HY-15141) and Doxorubicin (HY-15142A)
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Incubation Time:24 h
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Result:Synergistically potentiated paclitaxel-induced G2M arrest and induced cell death.
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Cell Line:MCF-7 cells
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Concentration:3.125, 6.25, 12.5, 25, 50 and 100 μM
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Incubation Time:24 h
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Result:Exhibited the greatest cytotoxic effect on MCF-7 cells, with an EC50 of 8.48 μM.
Did not kill the normal breast MCF-10A cells at 100 μM.
Exhibited the EC50 values against BT-483, MDA-MB-468 and ZR-75-1 to be 4.1, 5.2, and 6.7 μM, respectively.
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Cell Line:MCF-7
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Concentration:20 μM
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Incubation Time:24 h
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Result:Detected CASP7 activity only, and no activation of CASP3.
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Cell Line:Paclitaxel-resistant MCF-7 cells (7TR)
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Concentration:1.25, 2.5 and 5 μM alone or with STS and Doxorubicin
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Incubation Time:24 h
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Result:Decreased the levels of cleaved β-catenin and certain ABC transporter.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MCF-7 and MDA-MB-468 induced xenograft model established in NOD/SCID mice[1]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection (i.p.), once daily for 2 weeks
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Result:Led to a significant reduced tumor volume and induced an increase for apoptosis in tumor tissues.
Chemical Information
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Molecular Weight 411.45
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Formula C25H21N3O3
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SMILES
COC1=CC2=C(C3=C(N(N=C3C)C4=CC=CC=C4)N=C2C5=CC=C(O)C=C5)C=C1OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
XIAP-CASP7 PPI-IN-1 Related Classifications
HY-175177 Related Classifications
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