2. Apoptosis Stem Cell/Wnt
  3. Apoptosis Caspase β-catenin
  4. 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.

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XIAP-CASP7 PPI-IN-1 Chemical Structure

XIAP-CASP7 PPI-IN-1 Chemical Structure

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XIAP-CASP7 PPI-IN-1 Related Antibodies

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Description

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[1].

IC50 & Target[1]

Caspase-3

 

Caspase-7

 

Caspase-9

 

In Vitro

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 nM 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 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.

XIAP-CASP7 PPI-IN-1 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: Paclitaxel-resistant MCF-7 cells (7TR)
Concentration: 1.25, 2.5 and 5 μM alone or with Staurosporine (STS) (HY-15141) and Doxorubicin (HY-15142A)
Incubation Time: 24 h
Result: Synergistically potentiated paclitaxel-induced G2M arrest and induced cell death.

Western Blot Analysis[1]

Cell Line: MCF-7
Concentration: 20 μM
Incubation Time: 24 h
Result: Detected CASP7 activity only, and no activation of CASP3.

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7 cells
Concentration: 3.125, 6.25, 12.5, 25, 50 and 100 μM
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: paclitaxel-resistant MCF-7 cells (7TR)
Concentration: 1.25, 2.5 and 5 μM alone or with STS and Doxorubicin
Incubation Time: 24 h
Result: Decreased the level of cleaved β-catenin and certain ABC transporter.
In Vivo

XIAP-CASP7 PPI-IN-1 (Compound 643943) (20 mg/kg, i.p., once daily for 2 weeks) exhibits anti-tumor activity in a breast cancer mouse model[1].

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

Animal Model: MCF-7 and MDA-MB-468 induced xenograft model established in NOD/SCID mice[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 2 weeks
Result: Led to a significant reduced tumor volume and induced an increase for apoptosis in tumor tissues.
Molecular Weight

411.45

Formula

C25H21N3O3
SMILES

COC1=CC2=C(C3=C(N(N=C3C)C4=CC=CC=C4)N=C2C5=CC=C(O)C=C5)C=C1OC
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
References
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XIAP-CASP7 PPI-IN-1 Related Classifications

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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.

Keywords:

XIAP-CASP7 PPI-IN-1ApoptosisCaspaseβ-cateninBeta cateninQuinazolineCancer cellVEGFR2MCF-7 cellsInhibitorinhibitorinhibit

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